TW475927B - Arylalkyl-pyridazinone - Google Patents

Abstract

Arylalkylpyridazinone derivatives of the formula I and their physiologically acceptable salts in which R1, R2, R3, R4, R5 and Q have the meanings indicated in claim 1, show inhibition of phosphodiesterase IV and can be employed for the treatment of inflammatory processes and of allergies, asthma and autoimmune disorders.

Description

475927 A7 B7 V. Description of the invention (1) The present invention relates to compounds of formula I and their physiologically acceptable species 1 R2

(Please read the notes on the back before filling this page)

) = 〇 I

N Q-R5 where R 1 and R 2 are each independently Η or A, and R 3 and R 4 are each independently 0 H, 10 R 1 (D, — S — Ri 0, 1 S 0 — Ri 0. , -SO-R ,, -S〇2R10, Ha5, methyldioxy, -NO2, -NH2, -NHR10 or -NR10R1: L, R5 is phenyl, which is unsubstituted or R6 And / or single or double substitution of R7, Q is absent or is Ci-6 alkylene, R6 and R7 are each independently -NH2, -NR8R9, -NHRI0, -NRioRU, -N02, Ha ^, one CN, -0A, one COOH or one COOA, printed by R8 and R9 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs, each of which is Η, which can be replaced by 1 to 5 fluorine and / or chlorine atoms. 1-8 brewing group 'a (^ 〇〇 八, -30_ 八, a S02A, a CONH2, a CONHA, a CONA2, a CO-COOH, a CO-CO0A, a CO-CONH2, One CO — CONHA or one CO — C 0 NA 2, A is a Ci-e alkyl group, which can be from 1 to 5 fluorine and / or chlorine. The paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm). ) -4-475927 A7 _ B7 V. Invention Note (2) that the atom is substituted, and R 1Q and R 11 are each independently A, C 3-7 cycloalkyl, C4-8 methylidylcycloalkyl or C2-8 alkenyl, and H a is Fluorine, chlorine, bromine or iodine. Similar compounds are disclosed in DE 195 0 2 6 9 9.3 0 The present invention is based on the discovery of novel compounds which have useful properties and are especially useful for the production of drugs. Formula I The compounds and their hydrazones have useful pharmacological properties and good tolerability. In particular, they have an inhibitory effect on phosphodiesterase IV and can be used to treat asthma diseases. For example,? .0133 〇11, the method disclosed in human-eta allergologica 438-4 47 (1 97 1) was used to measure the anti-asthmatic effect. The compound additionally showed an inhibitory effect on the formation of TNF (tumor necrosis factor), and was therefore suitable for use in Treatment of allergies and inflammatory diseases, autoimmune diseases, and transplant rejection. It can also be used to treat memory diseases. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) Therefore, Compounds of formula I can be charged In human and veterinary medicine of pharmaceutically active compounds which may be further based purported to intermediates for the preparation of other pharmaceutically active compounds. Therefore, the present invention relates to a compound of formula I and its hydrazones, and a method for preparing the compound and its hydrazones, which is characterized in that the paper size of the compound of formula II is adapted to the Chinese National Standard (CNS) A4 specification (210 X 297 mm)- 5-475927 A7 B7 V. Description of the invention (

: 0

Among them, those defined by R 1 react with the compound of formula ΠΙ R 5 — Q — X

III (Please read the notes on the back before filling this page)

Γ · -L, where R5 and Q are as defined above, and X is chlorine, bromine or a reactive esterified OH group, or is characterized in that the compound of formula IV

R

0 R Ε Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

V wherein R1, R2, R3 and R4 are as defined above, and E is hydrogen or C ^ -4 alkyl, which is reacted with a compound of formula V

H2N — NH — Q — R, where Q and R5 are as defined above, or their characteristics are that by reducing nitro, alkylating or tritiating a primary or secondary moonyl or hydrolyzing cyano, the formula The R5 group in the compound I is converted into another paper size that is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm)-475927 A7 B7 V. Description of the invention (4) R5 group, and / or Let the compound corresponding to the formula I (but contain one or two free hydroxyl groups to replace R3 and / or R4) optionally with a compound of formula R3 — X — or R4 — X (wherein R3, R5 and X Is a reaction as defined above), and / or converts the base of formula I to hydrazone by interacting with an acid.

In the above and below, unless specifically stated otherwise, the definitions of the groups R1, R2, R3, R4, R5, Q and X are as defined in formulae I, II and III. A is an alkyl group. In the above formula, the alkyl group is suitably unbranched and has 1 to 6 carbon atoms, more suitably 1, 2, 3, or 4 carbon atoms, and more preferably a methyl group, further more preferably Suitably it is ethyl or propyl, and even more suitably is isopropyl, butyl, isobutyl, other-butyl or t-butyl, and also n-pentyl or isopentyl. The cycloalkyl group suitably has 3 to 7 carbon atoms and is suitably a cyclopropyl group or a cyclobutyl group, more preferably a cyclopentyl group or a cyclohexyl group, and further a cycloheptyl group. Printed by the Consumers' Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the notes on the back before filling this page) Methylcycloalkyl is suitably 4 to 8 carbon atoms, and more preferably Methylcyclo The propyl or methylidene cyclobutyl group is more preferably methylidylcyclopentyl or methylidylcyclohexyl, and further is methylidylcycloheptyl. Alkenyl is more preferably vinyl, 1- or 2-propenyl, 1-butenyl, isobutenyl, another butenyl, and further more preferably 1-pentenyl, isopentenyl Or 1-hexenyl. This paper size applies to China National Standard (CNS) A4 (210X297 mm) _-475927 Printed by A7 B7, Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (5) The alkylene group is more suitable It has a branched chain, and is more preferably a methylidene group or an ethylene group, and further preferably a propylene group or a butylene group. One of the R1 and R2 groups is more preferably hydrogen, and the other is more preferably propyl or butyl, and particularly suitably ethyl or methyl. R1 and R2 are further preferably both hydrogen. H a ί is more suitably fluorine, chlorine or bromine, and also iodine. The R3 and R4 groups may be the same or different, and are more preferably located at positions 3-or 4 of the benzene ring. It is, for example, hydroxyl groups, —S—CH3, —SO—CH3, —SO2CH3, fluorine, chlorine, bromine, or iodine, or methyldioxy, respectively, independently of each other. However, they are particularly suitably methoxy, ethoxy, propoxy, cyclopentyloxy, or fluoro-, difluoro- or trifluoromethoxy, or 1-fluoro-1,2 fluorine, respectively. Mono-1,2-difluoro-, 2,2-difluoro- 1,1,2,2-trifluoro- or 2,2,2-trifluoroethoxy. The R5 group is suitably phenyl. The phenyl is suitably mono- or di-substituted. Suitable substituents are gas, nitro, amine, acetamido, trifluoroacetamido, methoxy and / or chlorine, and also suitable are methanesulfonylamine, propylamino, 2-Methylpropanamido, isobutyramido and / or pentamidine, and more preferably, it is methoxycarbonylamino, acetochlor, urea and / or carboxyl. Q — R5 is more preferably fluorenyl, 2-, 3- or 4-mononitrofluorenyl, 2-, 3- or 4-monocyanofluorenyl, 2-, 3- or 4-monoamino ring, 2 —, 3 — or 4 monoethylaminobenzyl, 2 —, 3 — or 4 monotrifluoroethylamidinofluorenyl, 2 —, 3 — or 4 monomethoxyfluorenyl, 2 This paper size applies China National Standard (CNS) A4 Specification (210 X 297 mm) _ 8-(Please read the precautions on the back before filling this page) 475927 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A7 _B7 __ V. Description of the Invention (6) _, 3-or 4- monochlorobenzyl, further more suitably 2-, 3-, or 4-monosulfonylamidofluorenyl, 2-, 3-, or 4-propanamidofluorenyl , 2 —, 3 — or 4 mono (2-methylpropylamino) alkynyl '2' 3 or 4 monoisobutylamidinobenzyl, 2-, 3-or 4 monotetramethylammonium Benzyl, 2-, 3-, or 4-monomethoxycarbonylaminobenzyl, 2-, 3-, or 4-adenosyl '2-' 3-or 4-one condensed narrow group '2-' 3- Or 4-Alachlorpyridinyl, and more suitably also 2,3 -—, 2,4-a, 2,5— 2,6 —, 3, 4 —or 3,5-dinitro narrow group, 2,3-, 2,4 one, 2,5-, 2,6 —, 3,4 one or 3,5-two Aminobenzyl, 2,3-, 2,4 mono, 2,5 —, 2,6-, 3,4 mono or 3,5-diethylamidobenzyl'2,3 — 9 2 9 4 One 9 2 9 5 one 9 2 9 6 one, 3, 4 one or 3, 5 —bis (trifluoroacetamido) yl group, 2, 3 —, 2, 4, one '2, 5 —, 2, 6 —, 3,4 —or 3,5-dimethoxybenzyl, 2,3-, 2,4-mono, 2,5-, 2, 6-, 3, 4 —or 3,5-dichloro Book base, 2, 3 —, 2, 4 —, 2, 5 —, 2, 6 —, 3, 4 mono or 3, 5-dimethylsulfamidinobenzyl, 2, 3 —, 2, 4 — , 2,5—, 2,6—, 3,4 mono or 3,5-dipropionamidofluorenyl, 2,3 —, 2,4 —, 2,5 —, 2,6-, 3, 4 mono or 3,5-bis (2-methylpropylamido) fluorenyl '2, 3 —, 2,4 mono, 2, 5 —, 2' 6-, 3, 4 mono or 3, 5 — Diisobutylamidinoaminobenzyl, 2,3-, 2,4-, 2,5 —, 2,6 —, 3,4 —or 3,5 —dimethoxyaminoamino, 2 ,, 3 —, 2,4 1,2,5 —, 2,6 This paper size is applicable to Chinese National Standard (CNS) A4 (210 X 297 mm) _ 9-(Please read the precautions on the back before filling this page)- -Equipment · 475927 A 7 B7 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the invention (7) One, 3, 4 one or 3, 5—Dimethoxamine, 2, 3—, 2,4 —, 2, 5 —, 2, 6 —, 3, 4 mono or 3, 5-diureidobenzyl, 2, 3 —, 2, 4-, 2, 5-, 2, 6-, 3 , 4 — or 3, 5-two end of the foundation. Therefore, the present invention relates in particular to compounds of formula I, in which at least one of the groups has the meaning of a more suitable substituent as described above. Certain preferred compounds can be represented by the following formulae I a to I e, the formulae I a to I e are corresponding to the formula I, and the groups not described in detail are as defined by the formula I, but where In formula I a, R 1 is hydrogen, R 2 is hydrogen or A, and R 3 is 0 A; in formula I b, R 1 is hydrogen, R 2 is methyl or ethyl, and R3 and R4 are 0A; In formula I c, R 1 is hydrogen, R 2 is methyl or ethyl, R 3 is 0 A, and R 4 is C: -6 alkyl substituted with single, dione, or trifluoro, in formula I d R 1 is hydrogen, R 2 is methyl or ethyl, R3 and R4 are all 0R1Q, and R5 is single or double substituted phenyl; (Please read the precautions on the back before filling out this page) This paper size applies China National Standard (CNS) A4 specification (210X297 mm) _ 1〇_ 475927 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A7 B7 V. Invention description (8) R1 and R2 are hydrogen, R3 and R4 in formula Ie All are 0A, and are 0A; R5 is a single or disubstituted phenyl. The preparation of compounds of formula I and the starting materials for their preparation are by using known methods, such as those described in the literature (for example, such as Ho II be-n-Weyl, Methoden der organ i schen Ch emie [Methods of Organic Chemistry], Geory-Thieme-Verlag, Stu 11 -gart revealed standard procedures; however, it is specifically described in DE 195502699. 3), under known reaction conditions suitable for the reaction. In this case, a variation method known per se may be used, but it is not described in detail herein. In the compounds of the formulae II and IV, R 1, R 2,: R 3 and R 4 are as defined above, and particularly are more suitable groups. In the compounds of the formulae III and V, Q is more suitably a methyl group or an ethylene group, and is also a propylene group or an ethylene group. In compounds of formula IV, E is more preferably hydrogen, methyl or ethyl, and is also propyl or butyl. In the compounds of the formulae III and V, R5 is a more suitable group as defined above, and X is chlorine, bromine, a hydroxyl group or a reactive esterified hydroxyl group. If X is a reactive esterified hydroxyl group, it is more preferably C6 alkylsulfonyloxy (more preferably methylsulfonyloxy) or Cuoarylsulfonyloxy (more suitably Is phenyl- or p-tolylsulfonyloxy, and 2-sulfonylsulfonyloxy). If necessary, the starting material can also be formed in situ, so that the paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) -11-(Please read the precautions on the back before filling in this (Page) 475927 A7 B7 V. Description of the invention (9) It does not need to be separated from the reaction mixture, but can be further reacted immediately to form a compound of formula I. On the other hand, a stepwise reaction is also possible. More suitably, a compound of formula I can be formed by reacting a compound of formula II with a compound of formula III. In some cases, the starting materials of formulae II and III are known. If it is not known, it can be prepared by a method known per se. Titracones of formula II are described, for example, in Enr.  J.  Med.  Chem.  -ChimTherapeut.  644-650 (1977) 0 On the other hand, by methods known per se, such as described in the literature (for example, such as Houben-Weyl, Methoden der organischen C-hemie [Methods of Organic Chemistry], Georg-Thieme-Verlag, In the standard procedure disclosed by Stuttgart), the compound of formula III is prepared under reaction conditions known and suitable for carrying out the reaction. In this case, a variation method known per se may be used, but it is not described in detail herein. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page). In detail, in the presence or absence of inert solvents, at a temperature of about -20 to about 150 ° C Next, the reaction of 2, 3, 4, 5-tetrahydro-trapping well with the compound of formula III is preferably performed at a temperature between 20 and 100 ° C. Suitable inert solvents are, for example, hydrocarbons such as hexane, petroleum ether, benzene, toluene or xylene; chlorinated hydrocarbons such as trichloroethylene, 1,2-dichloroethane, carbon tetrachloride, chloroform or Dichloromethane; alcohols, such as methyl, ethyl, isopropyl, n-propyl, n-butyl, or t-butyl; ethers, such as diethyl ether; this paper is sized for China National Standard (CNS) A4 (210X297 mm) _ 12 _ 475927 A7 B7 _ 5. Description of the invention (10), isopropyl ether, tetrahydrofuran (THF) or dioxane; ethylene glycol ethers, such as ethylene glycol monomethyl ether or monoethyl ether (methyl ethylene glycol Or ethyl ethylene glycol), digly me; ketones, such as acetone or methyl ethyl ketone; ammonium, such as acetamide, dimethylacetamide, or dimethylformamide (DMF ): Eyes, such as acetonitrile; subcodes, such as dimethyl sulfoxide (DMSO): carbon disulfide; carboxylic acids, such as formic acid or acetic acid; nitro compounds, such as nitromethane or nitrobenzene; esters, such as ethyl acetate; or , The mixed solution of the solvents. Further, a compound of formula I can be produced by reacting a compound of formula IV with a compound of formula V. In particular, the reaction of the compound of formula IV with the compound of formula V is carried out in the presence or absence of an inert solvent and at a temperature as described above. In some cases, the starting materials of formulae IV and V are known. If it is not known, it can be prepared by a method known per se. Printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the notes on the back before filling this page) On the other hand, by methods known per se, such as described in the literature (for example, such as Houben-Weyl, Methoden der * organischen In C-hemie [Methods of Organic Chemistry], Georg-Thieme-Verlag, Stuttgart (standard procedures disclosed), the compounds of formulae IV and V are prepared under known reaction conditions suitable for the reaction. In this case, a mutation method known per se may be used, but it is not described in detail herein. Compounds of formula I can also be prepared, for example, by reducing a nitro group (for example, by hydrogenation with Raney nickel or palladium-nitrate in an inert solvent such as methanol or ethanol) to an amine group, or by hydrolyzing a cyano group to a carboxyl group. The R5 group in this paper applies the Chinese National Standard (CNS) A4 specification (210X 297 mm) -13-~ 475927 A7 B7 5. Description of the invention (11) Converted into another R5 group. It can also be conveniently used in an inert solvent of * dichloromethane or TH F, and / or in the presence of a base of * triethylamine or pyridine, and at a temperature of 60 to + 30 ° C, as is customary. This is accomplished by using a fluorenyl chloride or an acid anhydride to mash the free amine group, or using an unsubstituted or substituted alkyl halide to alkylate the free amine group. The compound corresponding to the formula I (but containing one or two free hydroxyl groups to replace R3 and / or R4) and the compound of the formula R3-X or R4-X (where R3, R4 and X are As defined above). The etherification of the hydroxyl group is performed by a method known per se, such as described in the literature (for example, Houben-Weyl, Methoden de r organischen Chemie [Methods of Organic Chemist-ry], Georg-Thieme-Verlag, Stuttgart) Standard procedure), that is, under known reaction conditions suitable for the reaction. In this case, a variation method known per se may be used, but it is not described in detail herein. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the notes on the back before filling this page) The acid can be used to convert the base of formula I to its related acid addition 加, for example, by The base is reacted in an amount with an acid in an inert solvent such as ethanol, and then evaporated. For this reaction, suitable acids are particularly those capable of generating physiologically acceptable maggots. Therefore, inorganic acids such as sulfuric acid; nitric acid; hydrohalic acids such as hydrochloric acid or hydrobromic acid; phosphoric acids such as orthophosphoric acid; aminosulfonic acids; organic acids, especially aliphatic acids, alicyclic acids, can also be used , Araliphatic, aromatic or heterocyclic mono- or polycarboxylic acids, sulfonic acids or sulfuric acids, such as formic acid, acetic acid, propionic acid, pivalic acid, diethylacetic acid, malonic acid, succinic acid, heptane Diacid, fumaric acid, maleic acid, lactic acid, this paper size applies Chinese National Standard (CNS) A4 (210X297 mm) _-475927 Printed by A7 B7, Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 12) Tartaric acid, malic acid, citric acid, gluconic acid, ascorbic acid, nicotinic acid, isonicotinic acid, methane mono or ethanesulfonic acid, ethanedisulfonic acid, 2-hydroxymonoethanesulfonic acid, benzene, para-one Toluenesulfonic acid, hydrazone mono- or disulfonic acid, and lauric acid. A hydrazone having a physiologically unacceptable acid, such as a picrate, can be used to isolate and / or purify a compound of formula I. On the other hand, if desired, a base (e.g., sodium hydroxide, potassium hydroxide, or rhenium carbonate) can be used to release the free base of the compound of formula I from the hydrazone of the compound of formula I. Compounds of formula I may contain one or more asymmetric centers. In this case, it usually exists in a racemic form. The resulting racemic product can be physically or chemically separated into its enantiomer by using a method known per se. Preferably, diastereomers can be generated from the racemic mixture by reaction with an optically active resolving agent. Of course, by the method described above, optically active compounds of formula I can also be obtained using optically active starting materials. Compounds of formula I include all stereoisomers and mixtures thereof, such as racemates. Class VIII also relates to the use of compounds of formula I and / or their physiologically acceptable properties to produce pharmaceutical preparations, in particular by non-chemical means. Herein, the compound of formula I and / or its physiologically acceptable compounds can be combined with at least one solid, liquid and / or semi-liquid excipient or adjuvant, and, as appropriate, one or more other active compounds , Together into an appropriate dosage form. '' The present invention also relates to the compound of formula I and its physiologically acceptable tincture. The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) -15 _ (Please read the precautions on the back before filling this page ) • Packing, 11 475927 A7 B7 printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs. 5. Description of the invention (13) A medicament for use as a phosphodiesterase [V inhibitor. The invention further relates to pharmaceutical formulations comprising at least one compound of formula I and / or one physiologically acceptable tincture. The preparation can be used as a human or veterinary drug. Suitable excipients are organic or inorganic substances that are suitable for enteral (e.g., oral) or parenteral or topical administration and do not react with the novel compound, such as water, vegetable oil, benzyl Alcohols, alkylene glycols, polyethylene glycols, triacetin, gelatin, carbohydrates such as lactose or starch, magnesium stearate, talc and petrolatum. Tablets, pills, coated tablets, capsules, powders, granules, syrups, juices or drops are particularly suitable for oral administration; suppositories are suitable for rectal administration; solutions, more suitable are oily or aqueous solutions, and suspensions Liquids, emulsions or implants are suitable for parenteral administration; and soft, 7jc paste or powder is suitable for topical administration. The novel compound can also be freeze-dried and the resulting freeze-dried product can be used to prepare, for example, injection preparations. The preparation can be sterilized and / or contain adjuvants such as lubricants, preservatives, stabilizers and / or wetting agents, emulsifiers, osmotic pressure, buffer substances, colorants, fragrances and / Or one or more other active compounds, such as one or more vitamins. The compounds of formula I and their physiologically acceptable pupae are useful for controlling diseases (wherein an increase in the amount of cyclic adenylate (CAMP) results in inhibition or prevention of inflammation and muscle relaxation). The compounds of the present invention are particularly useful in the treatment of allergies, asthma, chronic bronchitis, ectopic dermatitis, psoriasis and other skin diseases, as well as autoimmune diseases. Above and below, all temperature units are. C. In the following examples, the paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) -16-(Please read the precautions on the back before filling this page) 475927 A7 B7 5. In the description of the invention (14), a customary processing method means: if necessary, add water; if the stomach needs, adjust the p of the mixed solution to 10 according to the composition of the final product; extract with ethyl acetate or dichloromethane; Separate the organic phase, (please read the precautions on the back before filling out this page), dry on sodium sulfate, evaporate, and then purify by silica gel chromatography and / or. Example 1 To 4 · 7 Og of 6 — (3,4 -dimethoxyphenyl) — 2, 3,4,5 —tetrahydrodatrap — 3 —one dissolved in 15 Omj? Of THF () Suspension, add 2.24 g of potassium t-butoxide, and stir for 30 minutes. Then, add 4.  32 g of 4-mononitro-benzyl chloride, and the mixture was stirred at room temperature for 10 hours. Remove the solvent and dispose of (as before) the residue in the usual way. Obtained 2- (4-nitrobenzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydrodatrapne 3-ketone, 111. ?. 126. . Printed in a similar manner by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, by reacting 〃 with the following reactants to obtain the following products (ie, expressed as a reactant A% product '); and 3-Nitromethyl chloride: 2- (3-Nitromethyl) -6- (3,4-monomethoxybenzyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone, m.  p.  12 2 °; and 2—Nitrofluorenyl chloride: This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) —I?-475927 A7 B7 V. Description of the invention (15) Benzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone; and 2,3-dinitrofluorenyl chloride: 2- (2,3-dinitrobenzyl) -6- (3,4-dimethoxyphenyl) -2'3'4'5-tetrahydro tower coaxing a 3-ketone; and 2,4 one two Nitrofluorenyl chloride: 2- (2,4-dinitrobenzyl) -6- (3,4-dimethoxyphenyl) _2,3,4,5-tetrazine ; With 2-methoxybenzyl chloride: 2- (3-methoxymethoxy) -6- (3,4-dimethoxyphenyl)-2 '3' 4 '5-four-gas tower 3-ketone; and 4-monomethoxybenzyl chloride: 2- (4-methoxybenzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetra Discouragement of 3-11; and 2-chloromethyl chloride: 2- (2-chloromethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5- Tetrahydrotrap 3-ketone; printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) and 2,6-dichlorobenzyl chloride: 2- (2,6-dichlorobenzyl )-6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydroda-co-a 3-11; and 4-afluorobenzyl chloride: 2- (4- A) 6- (3,4-dimethoxyphenyl) -2,3,4,5-tetraaza-tower to coax a 3-keto I; and 4-carboxymethylfluorenyl chloride: This paper standard applies to China Standard (CNS) A4 specification (210X297 mm) -18-475927 A7 B7 V. Description of the invention (16) 2-(4-monocarboxybenzyl) 6-(3,4-dimethoxyphenyl) -2 , 3,4,5-tetrahydrodatrapone 3-ketone. Example 2 In a manner similar to Example 1, by making 6— (3,4—dimethoxyphenyl) —5—ethyl—2, 3, 4, 5—tetrahydrotrap — 3—one () Reacted with 4-nitrobenzyl chloride to obtain 2- (4-nitrobenzyl) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4 '5-tetrazolium coaxes a 3-ketone. In a similar manner, by reacting iB ′ with the following reactants, the following products are obtained (ie, expressed as a reactant ":% product >); and 3-nitrobenzyl Chlorine: 2- (3-nitro-narrow group) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydrodatrapeptone 3-ketone; Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) and 2-nitrobenzyl chloride: 2 — (2 —nitromethyl) — 6 — (3, 4 a Dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and 2,3-dinitrobenzyl chloride: 2- (2,3-di Nitrofluorenyl) -6- (3,4-dimethoxyphenyl) -5-ethyl_2,3,4,5-tetrahydro-3 trap-one; This paper size applies to Chinese national standards (CNS) A4 specification (210X297 mm) -19-475927 A7 B7 V. Description of the invention (17) and 2,4-dinitrobenzyl chloride: 2-(2,4-dinitrofluorenyl)-6 — (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5 — Hydrogen trap 3-ketone; and 2-methoxybenzyl chloride: 2- (2-methoxymethoxy) -6- (3'4-dimethoxyphenyl) -5-ethyl- 2,3'4,5-tetraazaphosphonium coaxes 3-3-benzyl and 3-methoxybenzyl chloride: 2- (4-methoxybenzyl) -6- (3,4-dimethoxy Phenyl) a 5-ethyl-2,3,4,5-tetrazol tower to cope with a 3-fluorene and 2-chloro; chloro: 2- (2-chlorobenzyl) -6 — (3,4 1-dimethoxyphenyl) -5-ethyl-2,3,4,5_tetrahydrodatrapeptone 3-ketone; and 2,6-dichlorobenzyl chloride: Consumer Cooperatives, Central Standards Bureau, Ministry of Economic Affairs Printed (please read the precautions on the back before filling out this page) 2 — (2, 6 — dichloromethyl) — 6 — (3, 4 —dimethoxyphenyl) — 5 — ethyl — 2, 3,4,5-tetrahydro-trap-a-3 ketone; and 4-amidinofluorenyl chloride: 2— (4-cyanoyl) —6— (3,4-dimethoxyphenyl) — 5 -Ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and 4-monocarboxyfluorenyl chloride: 2- (4-carboxyfluorenyl) -6- ( 3,4-dimethoxybenzene paper size applies to Chinese National Standard (CNS) A4 specifications (210X297 mm) -2-475927 A7 B7 V. Description of the invention (18) -based) 5-ethyl-2, 3,4,5_ four nitrogen towers coax one 3 — reward. Example 3 In a manner similar to Example 1, by making 6— (3,4-trifluoromethoxyphenyl) —5-ethyl-2,3,4,5-tetrahydrotrap —3— Ketone () reacts with 4-nitrobenzyl chloride () to obtain 2- (4-nitrofluorenyl) -6- (3-methoxy-4-trifluoromethoxyphenyl) -5- Ethyl-2,3,4,5-tetrahydrotrapping well 3-ketone 0 In a similar manner, by reacting with the reactants described below, the following products are obtained (ie, in% reactants ':% 产品 # The way is expressed); and 6- (3-methoxy-4 difluoromethoxyphenyl) -5-ethyl-2,3,4,5- 4-gas tower —Ketone: 2 — (4-nitrofluorenyl) — 6 — (3-methoxy-4 —difluoromethoxyphenyl) — 5 —ethyl-2, 3, 4, 5 — tetrahydro Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) -3 -ketones; and 6- (3-methyl'oxy-1, 4-methoxymethoxyphenyl) 5-Ethyl-2,3,4,5-tetrazol tower coaxes 3-keto I: 2— (4 Nitromethyl) -6- (3-methoxy-4-fluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrazol tower co-a 3-ketone; and 6- (3 —Difluoromethoxy_4 —methoxyphenyl) — 5 — This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) -21-475927 A7 B7 V. Description of the invention (19) Ethyl-2,3,4,5-Four gas towers coax a 3-Steel: 2- (4-Nitromethyl) -6- (3-Dimethoxymethoxy-4-methoxyphenyl) A 5-ethyl-2,3,4,5-tetrahydro-trap-a 3-ketone; and a 6- (3-trifluoromethoxy-4 4-methoxyphenyl) a 5-ethyl-2 , 3,4,5-tetrahydro-trap-a 3-ketone: 2- (4-mononitrobenzyl) -6- (3-trifluoromethoxy-4 4-methoxyphenyl) -5-ethyl -2,3,4,5-tetrahydro-3-well; and 6- (3-fluoromethoxy-4-methoxyphenyl) -5-ethyl-2,3,4,5 —The tetrazolium tower coaxes one to three—Remuneration: 2— (4-Nitromethyl) —6— (3-Fluoromethoxy—4—methoxyphenyl) —5 Ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and 6- (3-methoxy-4 4-ethoxyphenyl) -5-ethyl-2,3,4, 5 —Tetrazine coaxing — 3 — Brewing: 2 — (4 —Nitromethyl) — 6 — (3 —methoxy — 4 —B Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the Note: Please fill in this page again) oxyphenyl) a 5-ethyl-2,3,4,5-tetraazepine co-a 3-ketone; and 6- (3-methoxy a 4-methoxy Phenyl) _5 -ethyl-2,3,4,5-tetrahydro-trap-a 3-ketone: 2-(4-nitrophenyl)-6-(3-ethoxy-4 -methoxy Phenyl) -5 -ethyl -2,3,4,5 -tetrazole tower coke 3 -one; This paper size applies to China National Standard (CNS) A4 specifications (210X297 mm) -22-475927 A7 B7 V. Description of the invention (20) and 6- (3-hydroxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrazol tower coax 3 -Reward: 2-( 4-nitro-narrow group)-6- (3-Cyclo-4-methoxyphenyl) -5-Ethyl-2,3,4 , 5-tetragas tower to coax a 3-ketone; and 6- (4-methylsulfonylphenyl)-5-ethyl-2,3,4,5-tetraazepine to coax a 3-ketone: 2 — (4-nitrobenzyl) -6— (4-methylsulfonylphenyl) —5 —ethyl-2,3,4,5 —tetrazolium tower — 3 —fluorene; and 6_ (4 — (Methoxyphenyl) -5-ethyl-2,3,4,5-tetraazaphosphonium-coated 3-phosphonium: 2- (4-nitrobenzyl) -6- (4-methyloxy Phenyl) -5 -ethyl -2,3,4,5-tetrahydrocarbazine -3 -one; and 6-(3-cyclopentyloxy-4 -methoxy)-5 -ethyl- 2,3,4,5-tetraazaphosphonium coke a 3-ketone: 2- (4-nitrobenzyl) -6- (3-cyclopentyloxy-4_methoxyphenyl) -5-ethyl 1,2,3,4,5-tetrahydro-trap- printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 3 -one. Example 4 In the presence of Raney nickel, 4.6 g of 2- (4-nitrofluorenyl) -6- (3,4-dimethoxyphenyl)-2 'dissolved in 60m5 methanol was hydrogenated. 3,4,5-tetrahydropyridine coaxes a 3-ketone solution. The catalyst was removed by filtration, and the solution was concentrated. After recrystallization, the paper size is in accordance with Chinese National Standard (CNS) A4 (210X297 mm) -23-475927 A7 B7 V. Description of the invention (21) 2 — (4 —aminobenzyl) — 6 — ( 3,4 -dimethoxyphenyl) -2,3,4,5-four gas towers coax a 3-嗣, m · p · 1 8 4 ° 〇 In a similar manner, by hydrogenating the following reaction Products, in order to obtain the following products (that is, expressed as% reactant ':% product'); 2- (3-nitrofluorenyl) -6- (3,4-dimethoxyphenyl)- 2,3,4,5—Four gas towers coerce a 3— 嗣: 2— (3-aminobenzyl) -6— (3,4-dimethoxyphenyl) —2,3,4,5 -Tetrahydrodatrapeptone 3-ketone, m. p · 14 0 °; 2- (2-nitrobenzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5- four-gas towers coax a 3-ketone: 2 — (2-aminobenzyl) —6- (3,4-dimethoxyphenyl) —2,3,4,5-tetrahydro tower to coax 3-ketone; 2- (2,3-di Nitromethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone: Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please Read the notes on the back before filling in this page) 2 — (2,3-diaminofluorenyl) —6— (3,4-dimethoxyphenyl) —2,3,4,5-tetrahydro Datra-3-ketone; 2- (2,4-dinitrofluorenyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetraazafluorene 3-fluorene: 2- (2,4-diaminobenzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap- 3-ketone; 2— (4-Nitrofluorenyl) —6 — (3,4_dimethoxybenzene paper size applies to Chinese National Standard (CNS) A4 specifications (210X297 mm) -24-475927 A7 B7 Specify (22) yl) -5-ethyl-2,3,4,5-tetrahydrodatrapeptone 3-ketone: 2- (4-aminoamino) -6- (3,4-dimethylamine Oxyphenyl)-5-ethyl-2,3,4,5-tetragas tower coercion; 2- (3-nitrobenzyl) -6- (3,4-dimethoxyphenyl) ) A 5-ethyl-2,3,4,5-tetrahydro trap-a 3-ketone: 2- (3-aminoamino)-6- (3,4-dimethoxyphenyl)- 5-Ethyl-2,3,4,5-tetraazapyrene: one 3-reward 'm.  ρ.  4 9 °; 2-(2-nitromethyl)-6-(3,4-dimethoxyphenyl)-5-ethyl-2, 3, 4, 5-four gas towers coax a 3- Ketone 1: 2- (2-amino narrow group) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrazolium tower ; 2— (2,3-dinitromethyl) —6— (3,4-dimethoxyphenyl) —5—ethyl—2,3,4,5—tetrazolium tower—1 Ketones: 2— (2,3—diaminobenzyl) —6— (3,4—Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) Oxygen Phenyl)-5 -ethyl-2,3,4,5-tetrahydrodatrapeptone 3 -one; 2- (2,4-dinitromethyl)-6- (3,4-dimethoxy Phenyl) -5-ethyl-2,3,4,5-tetrahydrodatrapeptone-3 monoketone: 2- (2,4-diaminobenzyl) -6- (3,4-dimethyl (Oxyphenyl)-5 -ethyl-2,3,4,5-tetraazepine-co- 3 -one; This paper size applies to China National Standard (CNS) A4 (210X297 mm) -25-475927 A7 B7 V. Description of the invention (23) 2 — (4-nitronitro group) — 6 — (3-methoxyl 4 —difluoromethoxyphenyl) — 5_ethyl — 2 , 3,4,5-tetrahydro trap-3-ketone: 2- (4-aminoamino) -6- (3-methoxy-4-dimethoxymethoxyphenyl) -5-ethyl A 2 ′ 3 ′ 4 ′ 5 —four-gas tower co- 3 —one; 2 — (4-nitromethyl) — 6 — (3 —methoxy — 4 —difluoromethoxyphenyl) — 5-Ethyl-2,3,4,5-tetrahydro trap-3 Ketone: 2- (4-aminoamino) -6- (3-methoxy-4-dimethoxymethoxyphenyl ) A 5-ethyl-2,3,4,5-tetraaza-tower coke-3 -one; 2- (4-nitrobenzyl) -6- (3-methoxy-4-fluoromethoxy Phenyl)-5 -ethyl-2,3,4,5-tetrahydro-trap-3-ketone: 2-(4-amino narrow group)-6-(3 -methoxy-4 -fluoromethyl (Oxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the note on the back first) Please fill in this page again for the matters) 3 -ketone; 2-(4-mononitrofluorenyl) -6- (3-difluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3, 4,5 -tetrazolium tower -3-ketone: 2-(4-aminoamino)-6-(3-difluoromethoxy-4 -methoxyphenyl)-5-ethyl -2, 3,4,5 —tetrazole tower coke —3 —ketone; This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) -26-475927 A7 B7 V. Description of the invention (24) 2 — (4_ Nitromethyl) -6- (3-trifluoromethoxy-1. 4-monomethoxyphenyl)-5-ethyl-2,3,4,5-tetrahydro-3 -one: 2- (4-aminobenzyl) -6- (3-trifluoromethyl Oxy-4-methoxymethoxy) -5ethyl-2,3,4,5-tetraazepine-3-3-ketone; 2- (4-nitrobenzyl) -6- (3 _Fluoromethoxy-4-methoxyphenyl)-5-ethyl_2,3,4,5-tetrazol tower co-a 3-ketone: 2- (4-aminomethyl) -6- (3-Fluoromethoxy-4-methoxyphenyl)-5-ethyl-2,3,4,5-tetrakiazol-a 3-ketone; 2- (4-nitrobenzyl)- 6- (3-methoxy-4-ethoxyphenyl)-5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone: 2- (4-aminoamino) 6— (3—Methoxy—4—B Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) oxyphenyl) _5 —Ethyl-2,3, 4,5-tetrachloro tower coaxes a 3-ketone; 2- (4-nitromethyl) -6- (3-ethoxy-4-methoxyphenyl) -5-ethyl-2,3 , 4,5-tetrazolium tower co-a 3-ketone: 2- (4-aminoamino) -6- (3-ethoxy-4 4-methoxyphenyl) -5-ethyl-2,3 ， 4,5 —tetrazol tower co-a 3-ketone; This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) _ 475927 A7 B7 V. Description of the invention (25) 2 — (4-mononitro Book base) 6- (3-Hydroxy-4_methoxyphenyl) -5-Ethyl-2,3,4,5-tetrahydro-trap-3-ketone: 2-(4-aminobenzyl Group)-6-(3-hydroxy-4-methoxyphenyl)-5-ethyl-2, 3, 4, 5-tetrahydrodatra well-3-ketone; 2-(4-nitrobenzyl )-6- (4-Methanesulfonylphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone: 2- (4-aminoamidoxy) -6- (4-Methenylphenyl) —5 —ethyl-2,3,4,5-tetraazepine to coke 3-ketone; 2 — (4-nitrobenzyl) — 6 — (4 — (Methoxyphenyl) 5-ethyl-2,3,4,5-tetrakidone co-a 3-ketone: 2- (4-aminobenzyl) -6- (4 Methyloxyphenyl) —5 —ethyl-2,3,4,5-4-gas tower coaxed a 3-keto 1; 2 — (4-nitromethyl) — 6 — (3-cyclopentyl Oxy-4—methoxyphenyl) -5—ethyl-2,3,4,5-tetrahydro trap-3—one: Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the note on the back first) Please fill in this page for more details) 2 — (4-monoaminobenzyl) -6— (3-cyclopentyloxy-4—methoxyphenyl) -5—ethyl-2,3,4,5—tetra Hydrogen trap 3-ketone; 2- (3-nitrofluorenyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5- Tetrahydro trap- 3 -ketone: 2-(3-aminobenzyl) -6- (3-cyclopentyloxy-4)-This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ μ 475927 A7 B7 printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (26) methoxyphenyl)-5-ethyl-2, 3, 5-four Μ tower coaxed a 3-copper, ρ · 109ο; 2 — (4-nitrophenylethyl) -6_ (3,4-dimethoxy Phenyl) a 5-ethyl-2,3,4,5-tetragas tower to coax a 3-fluorene-2- (4-aminophenethyl) -6- (3,4-dimethoxybenzene A) 5-ethyl-2,3,4,5-tetrahydro-trap-a 3-ketone, 2- (4-nitrophenethyl) -6- (3,4-dimethoxyphenyl ) A 5-ethyl-2,3,4,5-tetrahydro-trap-a 3-ketone 2- (4-aminoaminophenethyl)-6- (3,4-dimethoxyphenyl)- 5-Ethyl-2,3'4,5-tetraazaphosphonium co-a 3-keto I 9 2- (3-nitrobenzyl) -6- (3-ethoxy-4 4-methoxybenzene A) 5 -ethyl-2,3,4,5 -tetrazol tower to cope with a 3 -ketone: 2-(3 -aminomethyl)-6-(3 -ethoxy-4 -methoxy Phenyl)-5 -ethyl-2,3,4,5-tetrahydro-trapping well 3 -one, m. p. 1120 0 Example 5 1 Og of 2- (4-Cyanosyl) -6- (3,4-dioxetylphenyl) -5-ethyl-2'3'4'5-tetrazolium tower I; _ | _ This paper size applies to China National Standard (CNS) A4 (210X297 mm) m 'ϋϋ —Lr--* I 1. ^ 1 1. ^ 1 n (Please read the precautions on the back before filling this page) Order printed by the Consumer Standards Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 475927 A7 B7 V. Description of the invention (27) 3-Ketone is added while stirring at the same time. It was dissolved in a cold solution of 1.2 g NaOH in 100 mi water, and the mixture was then stirred for 10 hours. Further, careful heating was applied and air flow passed through the solution. Subsequently, cold sulfuric acid and water were added. The mixture was treated in the usual manner, resulting in 2- (4-carboxycarboxybenzyl) -6- (3,4-dihydroxyphenyl) -5-ethyl-2,3,4,5-tetrahydroda Trap 3 -one Example 6 To 3.0 g of 2- (4-aminoaminobenzyl) -6- (3,4-dimethoxyphenyl) dissolved in 8 Omj? Of dichloromethane A 2,3,4,5-tetrahydro-trap well a 3-ketone () and 0.  A solution of 75 mj? Of pyridine was added with 1.0 g of butanyl chloride and then stirred for 1 hour. The solvent was removed and the residue was treated in the usual manner. After recrystallization, 2- (4-butyridinoaminofluorenyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap- 3-ketone was obtained , M.  ρ · 1 4 8. . In a similar manner, by reacting, D " with the following reactants to obtain the following products (ie, expressed as, reactant 〃:% product "); and acetyl chloride: 2— (4-Ethylamidofluorenyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone (CNS) A4 specification (210X 297 mm) IV I ill · n 1 ili I (Please read the notes on the back before filling in this page) Order -30-475927 Printed by A7 B7 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Invention description (28) m.  p.  18 3 °; with trifluoroacetamyl chloride: 2- (4-trimethylacetamide narrow group) -6- (3,4-dimethoxyphenyl) -2,3,4,5--4 Hydrogen trap-3-ketone, m.  p.  2 1 0 °; with methanesulfonyl chloride: 2- (4-methanesulfonylamine-narrow group) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrazine Tower coaxes a 3-ketone, m.  p.  1 3 8 °; with propionyl chloride: 2- (4-propanylaminomethyl)-6- (3,4-dimethoxyphenyl) _2,3,4,5-tetrazolium tower 3-ketone, m.  p.  17 6 °; with 2,2-dimethylpropanyl chloride: 2- (4-tert-butylcarbonylaminofluorenyl)-6- (3,4-dimethoxyphenyl)-2, 3, 4, 5 —tetrazolium tower coaxes 3 — 嗣 'm.  p.  15 5 °; with isobutylphosphonium chloride: 2- (4-isobutylphosphoniumaminofluorenyl) -6- (3,4-dimethoxyphenyl) -1,2,3,4,5-tetrahydroda Trap 3-ketone; and methyl chloroformate: 2- (4-methoxymethoxyaminomethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5 — Tetrahydro-trap-one 3-ketone; and Tetrazine chloride: This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ _ n 'I. . . . . . . . . 1 Him H m I (Please read the precautions on the back before filling out this page) 475927 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the Invention (29) 2— (4 Tetamidine Narrow Base ) A 6- (3,4-dimethoxyphenyl) -2,3,4,5-tetragas tower to cope with a 3-payer; and cyclopentanecarbamyl chloride: 2-(4-cyclopentylamino Formamyl benzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap- 3-ketone; and ethyl chloroformate: 2-(4 -ethyl Oxydiaminyl)-6-(3,4 -dimethoxyphenyl) -2,3,4,5-tetrahydro trap-3-ketone, m.  ρ · 1 4 7 0; and chlorantrol chloride: 2— (4- chloroformylbenzyl) —6— (3,4-dimethoxyphenyl) —2,3,4,5— The four nitrogen tower coaxes a 3-keto-1; and chloroformamide: 2- (4-adenosyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5 — Tetrahydrotrapeptone 3-ketone; and pentamidine chloride: 2- (4-pentanylaminomethyl)-6- (3,4-dimethoxyphenyl)-2, 3, 4, 5 — The four nitrogen tower coaxed a 3-keto I: and hexamethylene chloride: 2- (4-hexylaminomethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetra Azapine coaxes 3-keto-1; and pentafluoropropanyl chloride: 2- (4-pentafluoropropanamidofluorenyl) -6- (3,4-dimethoxyphenyl) -2,3 , 4,5-tetrahydro-trap-a 3-ketone. This paper size applies to China National Standard (CNS) A4 (210X297 mm) _ 32-(Please read the precautions on the back before filling out this page) 475927 Printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (30) In a similar manner, by making 2- (4-aminoamino) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3'4,5- Tetrahydrotrapone 3-ketone reacts with the following reactants to obtain the following products (ie, expressed as% reactants '; "products'); and acetamidine: 2 — (4 — Ethylaminomethyl) -6- (3'4-dimethoxyphenyl) _2,3,4,5-tetrahydrodatrapeptone 3-ketone; and trifluoroacetamidine: 2- (4 —Trifluoroacetamido) — 6 — (3,4-dimethoxyphenyl) — 2, 3, 4, 5 —tetrahydro trap — 3 — ketone, m.  p.  1 3 3 °; with methanesulfonyl chloride: 2— (4-methanesulfonylaminobenzyl) —6— (3,4—dimethoxyphenyl) —5—ethyl—2, 3, 4 , 5-tetrahydro-trap-a-3 ketone; and propanyl chloride: 2- (4-propanamidinyl) -6- (3,4-dimethoxyphenyl)-5-ethyl- 2,3,4,5-tetrahydro-trap-a 3-ketone, m · p · 8 1 0 and dimethylpropanyl chloride: 2-(4-tert-butyl-chitylamino)-6- (3,4—dimethoxyphenyl) -5—ethyl-2,3,4,5—tetrahydrodatrap This paper is sized for China National Standard (CNS) A4 (210X297 mm) _ 33 _ (Please read the notes on the back before filling this page)

LP 475927 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A7 B7 V. Description of the Invention (31) —3-ketone; and Butanyl Chloride: 2— (4-Butanamine Narrow Base) —6— (3, 4 One dimethoxyphenyl) one 5-ethyl-2,3,4,5- four gas tower to coax one 3-one, m · ρ · 1 1 7 °; and isobutyrine chloride: 2-(4 —Isobutylamidinoyl) — 6 — (3,4-dimethoxyphenyl) — 5 —ethyl — 2,3,4,5 —tetrahydrotrap — 3-ketone; and chloroformic acid Methyl esters: 2- (4-methoxymethoxyaminomethyl) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydrotrap A 3-ketone, mp1440; and pentamidine chloride: 2- (4-pentamylamino)-6- (3,4-dimethoxyphenyl) -5-ethyl-2, 3,4,5-tetrahydro-trap-3-ketone; and cyclopentanecarbamyl chloride: 2— (4-cyclopentylaminomethyl 1j? Yl) -6— (3,4-dimethoxy Phenyl)-5 -ethyl-2,3,4,5 -tetrahydro-trap well 3 -one, and ethyl chloroformate: 2-(4 -ethoxy Nylamino group)-6-(3,4-dimethoxyphenyl)-5-ethyl-2 '3 ^ 4, 5-tetrazolium tower, a paper size applicable to Chinese national standards (0? ) 8 4 specifications (210 '乂 297 mm) _9 / 1_ (Please read the notes on the back before filling out this page) 475927 A7 B7 V. Description of the invention (32) 3-ketone |, π · ρ · 1540; and Acetochlor: 2- (4--Aminopyrene narrow group) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro Trap-3-ketone; and chloroformamidine chloride: 2- (4-Ureabenzyl) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5 —Tetrahydro-trap-3-ketone; and pentamidine chloride: 2- (4-pentamylaminomethyl) —6- (3,4-dimethoxyphenyl) —5-ethyl-2, 3,4,5 —tetrahydrothrapy 3-ketone; and hexamethylene chloride: 2- (4-hexamethyleneaminomethyl) -6- (3,4-dimethoxyphenyl) -5— Ethyl-2,3,4,5-tetraazepine to coax 3_ ketone; and pentafluoropropanyl chloride: printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling out this page) 2— (4-pentafluoropropylamidobenzyl) —6— (3,4-dimethoxyphenyl) —5—ethyl-2, 3,4,5-tetraazepine coaxes a 3-ketone. In a similar manner, by making 2_ (4-aminomethyl) -6_ (3-ethoxy-4_methoxyphenyl) -5_ethyl_2'3'4, 5-tetrahydro Datra-3 ketone reacts with the following reactants to obtain the paper size applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) _milk 475927 A7 B7 V. Description of the invention (33) The following product ( That is, it is expressed in the form of a reactant product.) The Ministry of Economic Affairs and the Central Standard Employee Consumer Cooperative and Acetyl Chloride: 2— (4-Ethylaminomethyl) —6— (3——methoxyphenyl) — 5-Ethyl-2,3,4,5-3-ketone: and trifluoroacetamido chloride: 2- (4-trifluoroacetamidomethyl)-6-(-4 monomethoxyphenyl ) A 5-ethyl-2,3,4-datra-3-one; and methanesulfonyl chloride: 2- (4-methylsulfanylaminomethyl) -6- (3 4 -methoxyphenyl ) A 5-ethyl-2,3,4, trap-3-ketone; and propanyl chloride: 2- (4-mercaptoamino)-6_ (3-monomethoxyphenyl)-5 —Ethyl-2,3,4,5- 3 -one; and Butanidine : 2 — (4-Butylaminomethyl) -6— (3-ethoxy-4—methoxyphenyl) -5—ethyl-2,3,4,5—tetrahydroda —3 —Ketone; and isobutylammonium chloride: ethoxy-4, tetrahydrohydrogen trap 3—ethoxy, 5—tetrazol—ethoxy—5—tetrazol ethoxy—4—tetrazol tower ( Please read the precautions on the back before filling this page) This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) _% _ 475927 A7 B7 V. Description of the invention (34) 2 — (4_iso 丁 醯Narrow amino group)-6- (3-ethoxy-4 -methoxyphenyl)-5-ethyl-2,3,4,5-tetragas tower coke-3 -one; and methyl chloroformate Esters: 2- (4-methoxycarbonylaminobenzyl) -6- (3-ethoxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-4-gas tower Cocoa-3 ketone; and pentamidine chloride: 2- (4-pivalamidobenzyl) -6- (3-ethoxy-4-methoxyphenyl) -5-ethyl-2, 3,4,5 —tetrazolium hydrazone trap 3-ketone; and cyclopentanecarbamyl chloride: 2_ (4-cyclopentyl Methylformylbenzyl) -6- (3-ethoxy-4 ~ methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower trap 3-ketone; and chloroformic acid Ethyl ester: Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the notes on the back before filling this page) 2— (4_ethoxycarbonylaminobenzyl) —6_ (3 —ethoxy-4— (Methoxyphenyl)-5-ethyl-2,3,4,5-tetraaza-trap-3-3-one; and chloroform: 2- (4-metachlor benzyl) -6 — (3-Ethoxy-4-methoxyphenyl) —5-Ethyl-2,3,4,5-tetrahydro tower trap—3-ketone; and chloroformyl chloride: _. I_ This paper The standard is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) _475927 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A7 _B7___ V. Description of the invention (35) 2— (4—ureidofluorene-based) —6— (3-Ethoxy-4-methoxymethoxyphenyl) -5-ethyl-2,3,4,5-tetragas tower coax a 3-one ketone; and pentamidine chloride: 2-(4-pentamidine Aminofluorenyl) -6- (3-ethoxy-4-methoxy A) 5 -ethyl-2,3,4,5-four gas towers to cope with a 3-ketone; and hexamethylene chloride: 2-(4-hexamethyleneaminobenzyl)-6-(3-ethoxy -4 -methoxyphenyl) -5 -ethyl -2,3,4,5-four gas tower traps-3-ketone; and pentafluoropropanyl chloride: 2-(4-pentafluoropropanamido group (Methenyl) -6- (3-ethoxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydroda-co-3-ketone. In a similar manner, by making 2- (4-aminobenzyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2'3,4,5 -Tetrahydro trap-3-ketone reacts with the following reactants to obtain the following products (ie, expressed as% reactant ': >product'); and acetamidine: 2-(4 Acetylamidoyl) 6- (3-Cyclopentyloxy) A paper size applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 0〇-〇〇- · Φ Pack— (please first Read the notes on the reverse side and fill in this page) I Γ-ll I. Order-0 475927 Annex 2: Revised page of Chinese specification of Patent Application No. 85102257 March, 88, Republic of China 5. Fifth, the invention description (36) 4 Phenyl) a 5-ethyl-2,3,4,5-tetrahydro tower trap a 3-ketone; and trifluoroacetamyl chloride: 2-(4-trifluoroethylaminomethyl) -6 — (3-Cyclopentyloxy-4-methoxymethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydrodatrapeptone 3-ketone; mp · 162 °; and methanesulfonyl chloride z 2 — (4-methanesulfenylbenzyl) -6— 3-Cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-3 trap-one; and propanyl chloride: 2-(4-propanyl Aminomethyl) -6- (3-Cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydrodatrapeptone 3-π, π · ρ · 6 9. ; With 2,2-Dimethylpropionyl chloride: 2- (4-tert-butylcarbonylaminofluorenyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl 1,2,3,4,5 — Tetrahydro trap — 3-ketone; and butyl chloride: 2- (4-butanylaminomethyl) — 6 — (3-cyclopentyloxy — 4 —methyl (Oxyphenyl)-5 -ethyl-2,3,4,5 -tetrahydro trap-3 -one; and isobutyrine chloride: 2-(4-isobutylamidinoyl)-6- (3 —Cyclopentyloxy This paper is sized for China National Standard (CNS) A4 (210X 297 mm)) (Please read the notes on the back, and then fill in the items:: Write this page) Employees of the Central Bureau of Standards Printed by the cooperative-39-475927 A7 B7 V. Description of the invention (37)-4-methoxyphenyl)-5-ethyl-2, 3, 4, 5-four-gas tower coke-3-ketone; and chlorine Methyl formate: 2- (4-monomethoxycarbonylaminobenzyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5_tetra Air tower cooing—3-ketone; and Tetrazine Chloride: 2— (4-Tetrazine Methyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetraaza tower trap 3-ketone; and cyclopentyl Carbochloride: 2- (4-cyclopentylaminomethylbenzyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5 — Four air traps—3-ketone; and ethyl chloroformate: printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 2 — (4 —ethoxyamino Hexyl) —6 -— (3-cyclopentyloxy-4—methoxyphenyl) —5-ethyl-2,3,4,5—tetrahydrodawell—3-ketone, mp73 °; and Acetochlor: 2- (4-Metosaminomethyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5- Tetrachloromethane—3—ketone; and methamidyl chloride: 2— (4_ureidofluorenyl) —6— (3—cyclopentyloxy—4—paper size applicable to Chinese national standard (0 milk) 4 specifications (210 '/ 297 mm) _4〇_ 475927 A7 B7 5. Description of the invention (38) methoxyphenyl) One 5-ethyl-2,3,4,5-tetra-M tower coaxes a 3-ketone; with pentamidine chloride: 2- (4-pentanamidobenzyl) -6- (3-cyclopentyloxy A 4-methoxyphenyl group) a 5-ethyl-2,3,4,5-tetraaza tower trap-3 ketone; and hexamethylene chloride: 2- (4-hexamidineaminobenzyl)- 6 — (3 —cyclopentyloxy — 4 monomethoxyphenyl) — 5 —ethyl — 2,3,4,5 —tetrahydrotrap — 3 —one; and pentafluoropropanyl chloride: 2 — ( 4-Pentafluoroazetidinylamino) -6- (3-Cyclopentyloxy-4-methoxyphenyl) -5-Ethyl-2,3,4,5-tetrahydro tower trap-3 -ketone. In a similar way, by making 2- (4-aminophenethyl) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4, the Ministry of Economic Central Standard Printed by the Bureau ’s Consumer Cooperative (please read the precautions on the back before filling out this page) 5-Tetrahydro trap-3-Ketone reacts with the following reactants to obtain the following products (ie, a reactant ':% 产品 # The way of expression); with acetamyl chloride: 2 — (4-monoacetamidophenethyl) — 6 — (3,4 —dimethoxyphenyl) — 5 —ethyl — 2, 3,4,5 —tetrahydro-trap-one 3-ketone; 'ί The paper size is applicable to the Chinese National Standard (0?) 8-4 specifications (210, 乂 297 mm) Printed 475927 A7 B7 V. Description of the invention (39) and trifluoroacetamido chloride: 2 — (4-trifluoroacetamidophenethyl) — 6 — (3, 4-dimethoxyphenyl) — 5-Ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and methanesulfonyl chloride: 2— (4-methanesulfonylphenylene phenethyl) —6— (3,4— Dimethoxyphenyl) 5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and propanyl chloride: 2- (4-propanamidophenethyl) -6- (3,4-dimethyl (Oxyphenyl)-5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone: and butanyl chloride: 2- (4-butanylaminophenethyl)-6_ (3, 4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and isobutylphosphonium chloride: 2- (4-isobutylamidinylphenylethyl) ) -6— (3,4-dimethoxyphenyl) —5—ethyl—2,3,4,5-tetrahydrotrap —3—one; and methyl chloroformate: 2— (4 Monomethoxyepiaminophenylethyl) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydroda-co- 3 -one; Paper size applies to China National Standard (CNS) A4 specification (210X297 mm) -------- * --- install-(Please read the precautions on the back before filling this page) Order 475927

7 B 40 Chloride, Benzene, pentamidine, and pentamyl 2 4 phenylphenyloxymethane, tetrahydrogen I 5, _ 4 \ J /, radical 3 ethyl, benzene 2 radical I, ammonium pentamide I, special 5 6 3 4 3 Trap Benzamidine Monomethyl Ethyl Ammonia |: Group 5 Chloropentyl I: Fluorene Ring} Ester Carbon I Ethyl Ethyl 4 Benzene, Pentyl Alkyl Ketone •, Cyclic I Oxygen I Chloroketone and 2 Methyl 3 and ethyl 6 3 4 Hydrogen tetra 1 5, 4, 3, 2 (Please read the precautions on the back before filling out this page) 2 4 Ethylphenyl I Amino Ethyl Carbon I Oxy 5 Ethyl I: I Ν / chlorobenzylbenzene; oxalone methoxy I and methyl 3 2 radicals 3 4 6 5-well 4 tower, hydrogen 3 tetra well hydrogen tetra (-I 5 C3, I 4 \ 1 /, radical 3 ethyl, Benzene 2-Amino-Acetoacetone | Methyl 5: II Amine 4) {{Methyl 1 Benzene, Chloro-2 Ketones and Oxygen I A 3 3 4 Printed by the Consumer Cooperative of the Central Standards Bureau, Ministry of Economic Affairs, 2 Ethylbenzene Urea I 4 6 4 Methoxymethyl benzylchloride and 2 4 11 1 3-Tradahydrotetra-5, 4, 4, 3, 2 I ethyl ethylbenzene; Ketone oxygen | 5

Hydrogen tetrahydrogen I 5, I 4 \ 1 /, radical 3 ethyl, benzene 2 radical I, amino ammonium pentamide I 6 3 4 trap A 3 This paper size applies to China National Standard (CNS) A4 specifications (210X297 mm) _ 475927 A7 B7 V. Description of the invention (41) -one; and hexamethylene chloride: 2- (4-hexamidoaminophenethyl) -6- (3,4-dimethoxyphenyl) -5_ethyl Benzyl-2,3,4,5-tetrazolium towers cope with a 3 monoketone; and pentafluoropropanyl chloride: 2_ (4-pentafluoropropanamidophenethyl) -6- (3,4 —dimethyl (Oxyphenyl)-5-ethyl-2,3,4,5-tetrahydro-co--3 -keto0 In a similar manner, by making 2- (3-aminomethyl) -6- ( 3,4-dimethoxyphenyl)-5-ethyl-2,3,4,5-tetrahydro-trap- 3-ketone is reacted with the following reactants to obtain the following product (ie, Expressed in the form of% reactant ':% product'); and Acetyl chloride: Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 2— (3 — Ethylamine Amidino)-6- (3,4-dimethoxyphenyl A 5-ethyl-2,3,4,5-tetraazepine co-a 3-ketone; and trifluoroacetamido chloride: 2- (3-trifluoro ^ ethylamidomethyl)-6_ (3 , 4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone, mp1420 and methanesulfonyl chloride:

: I This paper size applies Chinese National Standard (CNS) A4 (210X297 mm) _ 475927 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (42) 2 — (3 — Methanesulfonamide Fluorenyl) -6- (3,4-dimethoxyphenyl) -5-ethyl-2,3,4,5-tetrazol tower co-a 3-ketone; and propionyl chloride: 2- (3 —Propanamido) — 6 — (3,4-dimethoxyphenyl) — 5 —ethyl — 2,3,4,5 —tetrazol tower co-a 3-ketone, m.p. 1 2 6 0; With butanyl chloride: 2-(3-butanylaminomethyl)-6- (3,4-dimethoxyphenyl)-5 -ethyl-2,3,4,5 —Tetrahydro-trap-a 3-ketone; and isobutylphosphonium chloride: 2- (3-isobutylamidoamino) -6- (3,4-dimethoxyphenyl) -5-ethyl- 2,3,4,5-Four gas towers cope with a 3-ketone; and methyl chloroformate: 2- (3-methoxycarbonylaminobenzyl) -6- (3,4-dimethoxyphenyl ) A 5-ethyl-2,3,4,5-tetrazol tower to coax a 3-ketone; and pivaloyl chloride: 2— (3 —Tentamylaminomethyl) — 6 — (3,4-dimethoxyphenyl) — 5 —ethyl — 2,3,4,5 —tetrazolidine — 3 —ketone; and cyclopentyl Alkyl chloride: _ I_ This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) _ 4 φ II (Please read the precautions on the back before filling this page) Order 475927 A7 B7 V. Description of the invention (43) 2_ (3-Cyclopentylcarbamoyl) -6- (3,4-dimethoxyphenyl) _5-ethyl-2,3,4,5-tetrahydrotrap-3 —Ketone, · and ethyl chloroformate: 2- (3-ethoxycarbonylaminobenzyl) —6- (3,4-dimethoxyphenyl) —5-ethyl—2 ^ 3 ^ 4 ^ 5 —The tetrazolium tower coaxes 3— 嗣, τη · ρ · 540; and chloroform: 2 -— (3-metamorphinomethyl) —6- (3,4-dimethoxyphenyl) One 5-ethyl-2,3,4,5-tetrahydro-trap-one 3-one ketone; and chloroformyl chloride: 2- (3-adenosyl) -6- (3,4-dimethoxy Phenyl) a 5-ethyl-2,3,4,5-tetrazol tower coax a 3-ketone; and pentamidine chloride: Printed by the Consumer Standards Cooperative of the Ministry of Standards of the People's Republic of China (Please read the notes on the back before filling this page) —Ethyl-2,3,4,5 —tetraazepine to cope with a 3 — ketone; and hexamethylene chloride: 2 ((3-hexamidine amino narrow group) — 6 — (3,4 —dimethoxy Phenyl) -5 -ethyl -2,3,4,5-tetrahydrodatrapeptone-3-ketone; and pentafluoropropanyl chloride: 2-(3-propfluoropropylamidinofluorenyl) -6 -(3,4 12 This paper size applies to Chinese National Standards (CNS) A4 specifications (210X297 mm) _ 475927 A7 B7 _ _ ㈣ Ⅴ. Description of the invention (44) methoxyphenyl) 1-5-B The base is a 2,3,4,5-tetrahydro-trap-a 3-ketone. In a similar way, by making 2- (4-aminoamino) -6- (3-fluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5 —Tetrahydro trap—3-ketone reacts with the following reactants to obtain the following products (ie, expressed as% reactant #% product "); and acetamidine: 2— (4 a Acetylaminobenzyl) -6- (3-fluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydrodatrapne 3-ketone; and Trifluoroacetamyl chloride: 2- (4-trimethoxyacetamidomethyl) -6- (3-fluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3,4 , 5-Tetrahydro trap 3 -one; Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) and Methanesulfonium chloride: 2-(4 Methanesulfonamide Narrow group) a 6- (3-fluoromethoxy-4 a methoxyphenyl) a 5-ethyl-2,3,4,5-tetrahydro trap-3 ketone; and propanyl chloride : 2- (4-propanamidinyl) -6- (3-fluoromethoxy -4 -methoxymethoxyphenyl) -5 -ethyl-2,3,4,5-tetrahydroda This paper is sized to the Chinese National Standard (CNS) A4 (210X297 mm)-47-475927 A7 B7 V. Description of the invention (45) Trap-3 -one; and butyl chloride: 2- (4-butyridinoaminofluorenyl)-6- (3-fluoromethoxy-1, 4-methoxyphenyl) -1 5-Ethyl-2,3,4,5-tetrahydrodatra-3-one; and isobutylphosphonium chloride: 2- (4-isobutylamidobenzyl) -6- (3-fluoromethoxy —4 —methoxyphenyl) —5—ethyl—2,3,4,5—tetragas trap—3—one; and methyl chloroformate: 2— (4-methoxycarbonylaminobenzyl ) A 6- (3-fluoromethoxy-4-methoxyphenyl) a 5-ethyl-2,3,4,5-tetrahydro-trap-a 3-ketone; and pivaloyl chloride: 2 — (4-Tetamylaminobenzyl) -6_ (3-fluoromethoxy-4—methoxyphenyl) -5—ethyl-2,3,4'5—tetraaza tower trap-3 — Ketone; Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) ) And cyclopentanecarbamyl chloride: 2- (4-cyclopentylcarbamoyl)-6- (3-fluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3 , 4, 5-tetrahydro tower coaxes a 3-ketone; with ethyl chloroformate: 2-(4-ethoxylated aminoamino)-6-(3-fluoromethoxy-4 -methoxy Phenyl) -5—Ethyl-2,3,4'5—Four paper sizes are applicable to China National Standard (CNS) A4 specifications (210X297 mm) _Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Chemical Industry and Economics 475927 A7 B7 V. Description of the invention (46) Hydrogen trap 3-ketone; and chlorfenone chloride: 2- (4-methyloxabenzylbenzyl) -6- (3-fluoromethoxy-4-4-methoxy Phenyl)-5 -ethyl-2,3,4,5-tetra-M tower trap-3 -one; and chloroformamide: 2-(4 -ureidomethyl) _6-(3-fluoromethoxy A 4-methoxy phenyl group) 5-ethyl-2,3,4,5-tetrazolidine co-a 3-ketone; and pentamidine chloride: 2- (4-pentanylaminomethyl) 6- (3-fluoromethoxy-4-methoxymethoxy) -5-ethyl 1,2,3,4,5- 4-tetranitropyrene trap 3-ketone; and hexamethylene chloride: 2- (4-hexamidine amino narrow group)-6- (3-fluoromethoxy-1 4- 1 (Methoxyphenyl) 5-ethyl-2,3,4,5-tetrahydro tower trap 3-ketone; and pentafluoropropanyl chloride: 2- (4-pentafluoropropanamidinylbenzyl) A 6- (3-fluoromethoxy-4, 4-methoxyphenyl), 5-ethyl-2, 3, 4, 5, 5-tetrahydro tower trap, a 3-one. In a similar manner, by making 2- (4-aminoamino) -6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl-2, this paper standard applies China National Standard (CNS) Α4 specification (210X297 mm) ^ -4y----- I ------ ^^ equipment-(Please read the precautions on the back before filling this page) Order 475927 Ministry of Economic Affairs Printed by the Consumer Standards Cooperative of the Central Standards Bureau. Reactant ':% product' is expressed in the way); and acetamidine chloride: 2- (4-acetamidoamino)-6- (3-dimethoxymethoxy-4-methoxyphenyl)- 5-Ethyl-2,3,4,5-Four air traps and 3-ketones; and trifluoroacetamido chloride: 2- (4-difluoroacetamidomethyl)-6- (3-di Fluoromethoxy-4, 4-methoxyphenyl), 5-ethyl-2,3,4,5, -tetrahydro tower trap, 3-ketone; and methanesulfonyl chloride: 2- (4-methanesulfonyl) Amine group) 6- (3-difluoromethoxy-4-methoxybenzene ) A 5-ethyl-2,3,4,5-tetrahydrothal — 3 -one; and propanyl chloride: 2- (4-propanamidobenzyl) -6- (3-difluoromethoxy -4-methoxymethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone; and butanyl chloride: 2- (4-butanylaminofluorenyl) A 6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap —3-ketone; _ I_ This paper size applies to China National Standard (CNS) A4 Specification (210X297mm) -〇1) (Please read the precautions on the back before filling this page) 475927 A7 B7 V. Description of the Invention (48) and Isobutyrium Chloride: 2 — (4 1 Isobutylammonium benzyl) -6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower trap 3-ketone ; And methyl chloroformate: 2- (4-monomethoxycarbonylaminobenzyl) -6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl-2,3, 4,5—tetrahydro tower coaxes a 3-ketone; and pivaloyl chloride: 2— (4-pentafluorenylamine ) -6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower trap 3-ketone; and cyclopentane carbon Ammonium chloride: 2- (4-cyclopentylaminomethylbenzyl) -6- (3-difluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5 — Tetrahydro trap-3—one; and ethyl chloroformate: Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs ^ n.------ I-.-*--M I-I (Please read first Note on the back page, please fill in this page again) 2— (4-ethoxycarbonylaminobenzyl) -6— (3-difluoromethoxy-4—methoxyphenyl) 5—ethyl-2, 3,4 '5 —tetrahydro tower to coax _ 3 _ ketones; and chlortoxanthine: 2-(4-chlortoxamine-based narrow group)-6_ (3 -difluoromethoxy-4 -methoxy Phenyl) -5-ethyl-2,3,4,5-tetrahydro tower coaxing a 3-ketone; This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) c, bl_475927 Ministry of Economic Affairs A7 B7 printed by the Consumer Standards Cooperative of the Central Bureau of Standards 5. Invention Description (49) : 2- (4-Ureabenzyl) -6- (3-Difluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro- 3-ketone; with pentamidine chloride: 2- (4-pentafluorenylaminofluorenyl) -6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl-2,3 , 4,5-tetraazapine-one 3-ketone; and hexamethylene chloride: 2- (4-hexamethyleneamino narrow group) -6- (3-difluoromethoxy-4 4-methoxyphenyl) One 5-ethyl-2,3,4,5-tetraaza-tower trap 3-ketone; and pentafluoropropanyl chloride: 2- (4-pentafluoropropylamidomethyl)-6- (3 — Difluoromethoxy-4, methoxymethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap-3-ketone. In a similar manner, by making 2- (4-aminomethyl) -6- (3-dimethoxymethoxy-4 dimethoxymethoxy) -5-ethyl-2,3,4 , 5 -tetrahydro trap-3-ketone reacts with the following reactants to obtain the following products (ie, expressed as% reactant;% product #); and acetamidine: I paper Standards are applicable to China National Standard (CNS) A4 specifications (210X297 mm) -52-(Please read the precautions on the back before filling out this page) ~ ^ Order · Order 475927 Printed by A7 B7 of the Consumer Standards Cooperative of the Central Standard Bureau of the Ministry of Economic Affairs Description of the invention (50) 2- (4-ethylamidoaminofluorenyl) -6- (3-trifluoromethoxy-4-methoxyphenyl) 5-ethyl-2,3,4 , 5-Four Gas Trap-3_one; and trifluoroacetamyl chloride: 2- (4-trifluoroacetamidomethylidene) -6- (3-trifluoromethoxy-4-methoxy Phenyl)-5 -ethyl-2,3,4,5-tetrahydropyrazol-3-one; and methanesulfonyl chloride: 2-(4 -methanesulfonylaminobenzyl) -6-(3 —Trifluoromethoxy-4 monomethoxyphenyl) -5 -2,3,4,5-tetrahydro-trap-a 3-ketone; and propanyl chloride: 2- (4-propanamidomethyl)-6- (3-trioxymethoxy-4 -methoxy Phenyl)-5 -ethyl-2,3,4,5-tetrahydro tower trap-3-ketone; and butyl chloride: 2-(4 -butyl fluorenylbenzyl)-6-(3 -tri Fluoromethoxy-4, 4-methoxyphenyl) 5-ethyl-2,3,4,5-tetrahydro tower coke-3, one ketone; and isobutyridine chloride: 2- (4-isobutyridine Narrow amino group)-6- (3-trifluoromethoxy-4-methoxyphenyl)-5-ethyl-2,3,4,5-tetrahydro trap-3 -one; and chlorine Methyl formate: This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) _ 53-(Please read the precautions on the back before filling out this page) 475927 Printed by A7 B7 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs V. Description of the invention (51) 2-(4-methoxymethoxyamino)-6-(3-difluoromethoxy-4-methoxyphenyl)-5-ethyl-2, 3 , 4,5_ Four gas tower traps and 3_ones; and Tetrazine chloride: 2— (4a Pentamidobenzyl)-6- (3-trifluoromethoxy-4-methoxyphenyl)-5-ethyl-2,3,4,5-tetrahydrodatrapeptone 3-ketone; With cyclopentanecarbamyl chloride: 2- (4-cyclopentylaminomethylmethyl)-6- (3-trifluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2 , 3,4,5 A tetrahydro tower trap a 3-ketone; and ethyl chloroformate: 2— (4-ethoxyalkylaminomethyl) -6— (3-trifluoromethoxy-4—methyl (Oxyphenyl)-5 -ethyl-2,3,4,5-tetrahydro tower coax a 3-ketone; and acetochlor: 2-(4-alachlor benzyl)-6- (3-trifluoromethoxy-4-methoxyphenyl) -5-ethyl-2'3,4,5-tetrahydro-3 trap-ketone; and chloroformyl chloride: 2-(4 _Ureidofluorenyl)-6- (3-trifluoromethoxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrazolidine-3 -one; and Pentamyl chloride: This paper size applies to China National Standard (CNS) A4 (210X297 mm) _ 54-(Please read the precautions on the back before filling (Write this page) 475927 A7 B7 V. Description of the invention (52) 2_ (4-pentamidoamino)-6- (3-difluoromethoxy-4-methoxyphenyl) -5-ethyl A 2,3,4,5-tetrahydro tower trap-3 ketone; and hexamethylene chloride: 2- (4-hexamethyleneaminobenzyl) -6- (3-trifluoromethoxy-4 monomethoxy Phenyl) a 5-ethyl-2,3,4,5-tetrahydro 11 hydrazone-3 ketone; and pentafluoropropanyl chloride: 2- (4-pentafluoropropylamidobenzyl) a 6_ (3-trifluoromethoxy-4_methoxymethoxyphenyl) -5_ethyl-2,3,4,5_tetrahydro-trap-3-ketone. In a similar manner, by making 2- (4-aminoamino) -6- (3-methoxy-4 4-fluoromethoxyphenyl) -5-ethyl-2,3,4,5 _ Tetrahydro trap- 3-ketone reacts with the following reactants to obtain the following products (ie, expressed as% reactant ': a product'); printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling out this page) and Acetyl Chloride: 2 — (4-Acetylamidomethyl) — 6 — (3 —Methoxy-4 —Methoxyphenyl) —5 —Ethyl-2,3,4,5-—tetrazolium towers cope with 3-ketones; and trifluoroacetamidine chloride: 2- (4-trineonylacetamidomethyl) —6- (3-methoxybenzyl Paper size applies Chinese National Standard (CNS) A4 specification (210X297 mm) _ 55-475927 Printed by A7 B7, Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (53) 4-methoxyphenyl) 5 —Ethyl-2,3,4,5 —tetraaza-trap- 3-ketone; and methanesulfonyl chloride: 2 — (4 -methanesulfonylaminomethyl) — 6 — (3 —methoxyl-4 — (Methoxyphenyl)-5-ethyl-2,3,4,5-tetrahydro tower coke-3 -one: and propionyl chloride: 2-(4-propionamidofluorenyl)-6-( 3-methoxy-4, 4-methoxymethoxyphenyl) 5-ethyl-2,3,4,5-tetraaza-trap-3-3-one; and butanyl chloride: 2- (4-butanylamino) Benzyl)-6- (3-methoxy-4-fluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro trap-3-ketone; and isobutyryl chloride : 2- (4-isobutylamidinylbenzyl) -6- (3-methoxy-4-fluoromethoxyphenyl) 5-ethyl-2,3,4,5-tetrahydro tower Coax ... 3-ketone; and methyl chloroformate: 2- (4-methoxycarbonylaminofluorenyl)-6- (3-methoxy-4 -fluoromethoxyphenyl) -5-ethyl-2 , 3, 4, 5—tetrahydro tower trap—one 3-ketone; and pivaloyl chloride: 2 -— (4-tetramethylpyridinylamino) —6- (3-methoxy—a paper size applicable to China National Standard (CNS) A4 Specification (210X297mm) _%-(Please read the precautions on the back before filling this page) •-1—1 8 I---- 1 -0 pack ·

1T 475927 A7 B7 V. Description of the invention (54) 4 monofluoromethoxyphenyl) _5_ethyl-2,3,4,5-tetrahydro-trap well 3_one; and cyclopentanecarbamyl chloride : 2- (4-Cyclopentylaminomethylsulfanyl) -6- (3-methoxy-4 4-fluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro Datra-3 ketone; and ethyl chloroformate: 2_ (4-ethoxystidinylamino)-6- (3-methoxy-4 monofluoromethoxyphenyl) -5-ethyl -2, 3, 4, 5-tetrahydro tower trap-3-ketone; and formazan chloride: 2-(4-formazanylmethyl)-6-(3-methoxy-4-gas (Methoxyphenyl)-5-ethyl-2,3'4,5-tetraazapine_3-ketone; and methylformyl chloride: printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the back first) For the matters needing attention, please fill in this page again) 2 — (4 —ureidomethyl) — 6 — (3 —methoxy — 4 —fluoromethoxyphenyl) — 5 —ethyl — 2, 3, 4, 5 —Tetrazolium co-a 3-ketone; and pentamidine chloride: 2 — (4-pentamethylaminomethyl) — 6 — (3 Methoxy-4, 4-fluoromethoxyphenyl), 5-ethyl-2,3,4,5-tetrahydro tower trap, 3-ketone; and hexamethylene chloride: 2- (4-hexamidineamino) Yenyl) — 6 — (3 —methoxy — 4 _ I_ This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm) _ 57-475927 A7 B7 5. Description of the invention (55) monofluoromethoxy Phenyl)-5 -ethyl-2,3,4,5-tetrahydroda- 3 -one; and pentafluoropropanyl chloride: 2-(4-pentapropoxyamidomethyl)-6 — (3-methoxy-4-fluoromethoxyphenyl) —5-ethyl-2,3,4,5-tetrahydro tower trap—3-ketone. In a similar manner ^ by making 2- (4-aminoamino) -6- (3-methoxy-4_difluoromethoxyphenyl) -5_ethyl-2, 3, 4, 5-tetrahydro trap-3-ketone reacts with the following reactants to obtain the following products (ie, expressed as% reactant ':% product'); and acetamidine: 2-(4 Monoethylaminomethyl) -6- (3-methoxy-4-difluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap- 3-ketone Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) and trifluoroacetamido chloride: 2— (4-trifluoroacetamidofluorenyl) —6— (3 _Methoxy-4—dimethoxymethoxyphenyl) -5—ethyl-2,3,4,5—tetrahydro-trap-3-ketone; and methanesulfonyl chloride: 2— (4-methyl Sulfonamido) -6- (3-methoxy-4-difluoromethoxyphenyl) -5-ethyl-2,3,4,5—Four paper standards are applicable to Chinese national standards ( CNS) A4 specification (210X297mm) _ 58-475927 A7 B7 V. Invention theory (56) A gas tower coaxes a 3-ketone; and propanyl chloride: 2- (4-propanamidobenzyl) -6- (3-methoxy-4 difluoromethoxyphenyl) -5 —Ethyl-2,3,4,5—Four gas tower traps—3-Ketone; and Butanyl chloride: 2- (4-Butylaminomethyl) —6— (3-Methoxy—4— Difluoromethoxyphenyl)-5 -ethyl-2,3,4,5 -tetrahydrooranium trap-3 -ketone; and isobutylphosphonium chloride: 2-(4-isobutylamidoaminobenzyl ) A 6- (3-methoxy-4 difluoromethoxyphenyl) a 5-ethyl-2,3,4,5-tetrahydro-trap-a 3-ketone; and methyl chloroformate: 2- (4-methoxymethoxyaminomethyl) -6- (3-methoxy-4-difluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower Well one 3-ketone; printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) and Tetrazine Chloride: 2-(4-Tetrazolamine-based Book Base)-6 — (3-methoxy-4-difluoromethoxyphenyl)-5-ethyl-2,3,4,5 — Hydrogen trap—3-ketone; and cyclopentanecarbamyl chloride: 2— (4-cyclopentylcarbamidine 1-yl) —6 -— (3-methoxy—4—difluoromethoxyphenyl) — 5-Ethyl-2,3,4,5 This paper is again applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) _ 59-475927 A7 B7 V. Description of the invention (57) A tetrahydrotrap trap 3 —Ketone; and ethyl chloroformate: 2- (4-ethoxymineamino narrow group) —6- (3-methoxy-4—difluoromethoxyphenyl) and 5-ethyl-2, 3,4,5 — Tetrahydro trap_3_ ketone; and chlorfenone chloride: 2— (4- oxametaminobenzyl) —6— (3-methoxy-4—difluoromethoxy Phenyl) -Ethyl-5,2,3,4,5-Four gas tower traps 3-ketones; and chloroformyl chloride: 2- (4-adenosyl) -6- (3-methoxy 4- (4-difluoromethoxyphenyl)-(5-ethyl-2,3,4,5-tetrahydro-3) -ketone; and pentamidine chloride: 2- (4-pentamylamino) A) 6- (3-methoxy-4-dimethoxymethoxyphenyl) -5-ethyl-2,3,4,5-tetraaza Tower trap —3 — Ketone; Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) and hexamethylene chloride: 2 — (4 —Hexamine amino group) — 6 — (3-methoxy-4, 2-dimethoxymethoxyphenyl) 5-ethyl-2,3,4,5-tetraaza- trap-3 -one; and pentafluoropropanyl chloride: 2- ( 4-Pentafluoropropanamidofluorenyl) -6- (3-methoxy-4 difluorofluorophenyl) 5-ethyl-2,3,4,5 — This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ go _475927 A7 B7 V. Description of the invention (58) Four gas towers coax a 3-ketone. In a similar manner, by making 2- (4-aminoamino) _6_ (3-methoxy-4_trifluoromethoxyphenyl)-5-ethyl_2, 3, 4, 5 —Tetrahydro-Trap — 3-ketone reacts with the following reactants to obtain the following products (ie, expressed as a reactant ':% product'); and acetamidine chloride: 2_ (4_ethyl Fluorenylbenzyl) -6- (3-methoxy-4-trifluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower trap-3 -one; and Trifluoroacetamyl chloride: 2- (4-trifluoroacetamidobenzyl) -6- (3-methoxy-4-4-trifluoromethoxyphenyl) -5_ethyl_2,3,4 , 5 — Tetrahydro tower coaxing a 3-ketone; and mesosulfuron chloride: printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) Narrow group) a 6- (3-methoxy_4-trifluoromethoxyphenyl) a 5-ethyl-2,3,4,5-tetrahydro trap-3 ketone; and propyl hydrazone Chlorine: 2- (4-propanamidobenzyl) -6- (3-methoxy-4, trifluoromethoxyphenyl) 5 —Ethyl-2,3,4,5 —Tetrahydrotraptra 3 —one; _ i__ This paper size applies to Chinese national standard (〇 奶) person 4 specifications (210 '乂 297 mm) _61_ 475927 A7 B7 V. Description of the invention (59) and Butanyl chloride: 2-(4-Butanylaminofluorenyl)-6-(3-methoxy-4-trifluoromethoxyphenyl)-5-ethyl- 2,3,4,5-tetrahydrothalada-3 ketone; and isobutylphosphonium chloride: 2- (4-isobutylamidobenzyl) -6- (3-methoxy-4 4-trifluoro Methoxyphenyl)-5 -ethyl-2,3,4,5-4-gas tower traps 3-ketones; and methyl chloroformate: 2-(4-methoxymethoxyaminomethyl)- 6_ (3-methoxy-4-4-dimethoxymethoxyphenyl)-5-ethyl-2,3,4,5_tetrahydro tower trap-3_one; and pivalamyl chloride: 2-(4 —Pentamidine group — 6 — (3-methoxy-4_trifluoromethoxyphenyl) — 5-ethyl-2, 3, 4, 5 — tetrahydrotrap — 3 — Ketones; and Cyclopentane Carbochloride: Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the note on the back first) Please fill in this page for the matters needing attention) 2— (4-Cyclopentylcarbamobenzyl) —6— (3-Methoxy-4—Trifluoromethoxyphenyl) —5—Ethyl-2,3, 4,5 -tetrakidone co-a 3-ketone; and ethyl chloroformate: 2-(4-ethoxyoxyamino narrow group)-6- (3-methoxy-4 -trifluoromethoxy Phenyl)-5 -ethyl-2,3,4,5-tetrahydro-trap trap 3 -one; This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _-475927 A7 B7 Description of the invention (60) and chlorantrol chloride: 2-(4-monomethoxamidinyl)-6-(3-methoxy-4-trifluoromethoxyphenyl)-5-ethyl-2 , 3,4,5-tetrahydrofluorene trap 3-ketone; and chloroformyl chloride: 2- (4-adenylyl) -6- (3-methoxy-4 difluoromethoxy Phenyl) -Ethyl-5,2-, 3,4,5-tetrahydrothalkan-3; one; and pentamidine chloride: 2- (4-pentamidoaminomethyl) -6- (3-methoxy-1 4-trifluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro tower co-a 3-ketone; and Ammonium chloride: 2- (4-hexamethyleneaminobenzyl) -6- (3-methoxy-4-4-trifluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro Tower coercion 3-keto; and pentafluoropropylchloride: Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) 2 — (4 —pentafluoropropylamidobenzyl ) —6 -— (3-methoxy-4-trifluoromethoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap- 3-ketone. In a similar manner, by making 2- (4-aminoaminobenzyl) -6- (3-ethoxy-4-methoxyphenyl) -2,3,4,5-tetrahydro- 3 —Ketone, m · ρ · 12 0 ° reacts with the following reactants The paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) -63-475927 A7 B7 5. Description of the invention (61), In order to obtain the following product (that is, expressed as | Reactant #: 1 产品 #); and acetamidine chloride: 2-(4-ethylamidoamino narrow group)-6-(3-ethoxy_ 4-methoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone, m.p. 1 70 °; and trifluoroacetamidine: 2- (4-trifluoroethyl Fluorenylamino) -6- (3-ethoxy-4-methoxyphenyl) -2,3,4,5-tetraazaphosphonium co-a 3-ketone; and mesylsulfonyl chloride: 2 — (4-Methanesulfonamidobenzyl) —6— (3-Ethoxy-4—methoxyphenyl) —2,3,4,5—tetrazolium towers—3— 嗣 9 and propyl醯 Chlorine: Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back first) (Fill in this page again) 2 — (4-Propanamido) — 6 — (3-Ethoxy-4 —methoxyphenyl) — 2, 3, 4, 5 — Tetrahydrotrap — 3 —Ketone; and Butanyl chloride: 2- (4-Butanamidofluorenyl) —6- (3-ethoxy-4—methoxyphenyl) —2 ′ 3 ′ 4 ^ 5 —tetrazolium tower Co-a 3-keto 1; and isobutylphosphonium chloride: 2- (4-isobutylamidoaminofluorenyl) -6- (3-ethoxy-4-methoxyphenyl) -2,3,4 ， 5 —Tetrahydro trap—3—Ketone The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) _ _ 475927 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (62 ), And methyl chloroformate: 2-(4-methoxymethoxyamino narrow group)-6-(3-ethoxy-4 -methoxyphenyl)-2, 3, 4, 5-tetra Hydrogen traps 3-ketones; and pentamidine chloride: 2- (4-pentamidine amino narrow group) -6- (3-ethoxy-4-methoxyphenyl) -2,3,4 , 5-tetrahydro-trap-a 3-ketone 9 and cyclopentanecarbamyl chloride: 2- (4-cyclopentylcarbamidine ) A 6- (3-ethoxy-4 4-methoxyphenyl) -2,3,4,5-tetrakidone-coated _3 monoketone; and ethyl chloroformate: 2-(4-ethyl Oxoylaminomethyl) -6- (3-ethoxy-4-methoxyphenyl) -2,3,4,5-tetragas towers co-a 3-ketone, m · ρ · 1 2 8 0; with chloroform: 2 -— (4-monomethoxenyl) —6- (3-ethoxy-4—methoxyphenyl) —2, 3, 4, 5—tetra Hydrogen trap 3-ketone 9 and chloroformyl chloride: 2-(4-ureidofluorenyl) 6-(3-ethoxy-4 -methoxyphenyl) _2,3,4,5- Tetrahydro trap-3_one; This paper size is applicable to China National Standard (CNS) A4 (210X297mm) _ 65 _ (Please read the precautions on the back before filling this page) 475927 A7 ^ __ E_ — V. Invention Explanation (63) and pentamidine chloride: 2- (4-pentamylaminofluorenyl) -6- (3-ethoxy-4 ~ methoxymethoxyphenyl) -2,3,4,5-tetrahydro Coaxing a 3-ketone; and hexamethylene chloride: 2- (4-hexamethyleneaminobenzyl) -6- (3-ethoxy -4-Methoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone; and pentafluoropropanyl chloride: 2- (4-pentafluoropropylamidobenzyl) -6 — (3-Ethoxy-4—methoxymethoxyphenyl) —2,3,4,5—tetrahydro 11 hydrazone—3—one 0 In a similar manner, by making 2- (4-amino Fluorenyl)-6-(3-cyclopentyloxy-4-methoxyphenyl)-2 '3' 4, 5-tetrahydrodatrap-3-ketone reacted with the following reactants to obtain the following The product described above (ie, expressed as% reactant 〃: a 产品 #); and ethyl chloride: printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) 2 — (4-Ethylaminomethyl) -6- (3-Cyclopentyloxy-4-methoxymethoxyphenyl) -2,3,4,5-tetrahydro-trapping well 3-ketone, and trifluoro Acetyl chloride: 2- (4-trifluoroacetamidobenzyl) -6- (3-cyclopentyloxy-4 monomethoxyphenyl) -2,3,4,5-tetrahydrodatra One 3-ketone; This paper size applies to China National Standard (CNS) A4 specification (210X2 97mm) _ _ Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 475927 A7 B7 V. Description of the invention (64) and methanesulfonyl chloride: 2 — (4 —methanesulfonyl benzyl) — 6 — (3 _Cyclopentyloxy-4-methoxyphenyl) -2,3,4,5-tetrahydrot trap-3-ketone; and propionyl chloride: 2- (4-propionylaminomethyl)- 6-(3-Cyclopentyloxy-4-methoxyphenyl)-2,3,4,5-tetrahydro-trap-a 3-ketone and 2,2-dimethylpropanyl chloride: 2-( 4-tert-butylcarbonylaminofluorenyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone; and butyl Fluorine: 2- (4-butamidinomethyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone With isobutylphosphonium chloride: 2- (4-isobutylamidinylbenzyl) -6- (3-cyclopentyloxy-4 4-methoxyphenyl) -2,3,4,5-tetraaza tower Coax a 3-ketone; and methyl chloroformate: 2- (4-methoxymethoxyaminomethyl) -6- (3-cyclopentyloxy-4-methyl Phenyl) -2,3,4,5-tetrahydro-trap-3-ketone; This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ _. .......- i— 11-m. —1 111-I ——- ϋ (Please read the notes on the back before filling out this page) Order 475927 Printed by the Consumers Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (65) and Pentamidine Chloride: 2- (4-Pentamidine amino narrow group) -6- (3-Cyclopentyloxy-4-methoxyphenyl) -2,3,4,5-tetrazolium A 3-ketone; and cyclopentanecarbamyl chloride: 2- (4-cyclopentylaminomethylformyl)-6- (3-cyclopentyloxy-4 4-methoxyphenyl) -2,3 , 4, 5-tetrazolium tower coaxes a 3-ketone; with ethyl chloroformate: 2- (4-ethoxyminylamino)-6- (3-cyclopentyloxy-4-methoxybenzene A) 2, 3, 4, 5 —tetrazine coaxing a 3 -keto; and chloroform chloride: 2 — (4-amethoxamine benzyl) — 6 — (3-cyclopentyloxy — 4-monomethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone; and chlorine Formamidine chloride: 2-(4-ureidofluorenyl)-6-(3-cyclopentyloxy-4-methoxyphenyl)-2 ^ 3,4,5-tetrazolium tower coke 3-Li ; With pentamidine chloride: 2- (4-pentamylaminobenzyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -2,3,4,5-tetrahydro-trap- 3 —Ketone and hexamethylene chloride: This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm) _Ming-I. I —T · ―--* 1 -— -—-- (Please read first Note on the back, please fill in this page again), tr 475927 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (66) 2 — (4 —Hexamine base group) — 6 — (3 — Ring Amyloxy-4 -methoxyphenyl) -2,3,4,5-tetrahydrotrap -3-ketoline and pentafluoropropanyl chloride: 2-(4-pentafluoropropanamido narrow group ) -6- (3-Cyclopentyloxy-4-methoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone. In a similar manner, by letting 2_ (4-aminophenethyl) _6_ (3'4-dimethoxyphenyl)-2'3'4'5-tetra-portal trap trap 3-one with The following reactants are reacted to obtain the following products (ie, expressed as a reactant ':% product'); and acetamidine chloride: 2-(4-ethylaminoaminophenethyl)-6 — (3,4-dimethoxyphenyl) —2,3,4,5—tetrazolium coke—3—fluorene; and trifluoroacetamido chloride: 2— (4-trifluoroacetamidoaminobenzene) (Ethyl)-6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap- 3-ketone; and mesylsulfonium chloride: 2- (4-methaneamine Phenylethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro tower trap-3-one; and propionyl chloride: 2- (4-propanol Amine Phenethyl) _6_ (3 '4 — One paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) _ 69 _ (Please read the precautions on the back before filling out this page) • — ^ Binding and printing printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 475927 A7 B7 V. Inventions Ming (67) oxyphenyl) _2,3,4,5-tetrahydropyridine trap 3-ketone; and butanyl chloride: 2- (4-butyridinoaminophenethyl) -6- (3, 4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone; and isobutylphosphonium chloride: 2- (4-isobutylphosphoniumaminophenethyl)-6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone; and methyl chloroformate: 2- (4-methoxycarbonylaminophenethyl) A 6- (3 ^ 4-dimethoxyphenyl) _2,3,4,5-tetragas tower to coax a 3-ketone; and pivaloyl chloride: 2_ (4-pivaloaminophenylphenethyl) ) A 6- (3,4-dimethoxyphenyl) -2,3,4,5-tetraazapyrene 1-3-ketone; and cyclopentanecarbamyl chloride: 2- (4_cyclo Amylaminotolylethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone; and ethyl chloroformate: 2- (4 Monoethoxycarbonylaminophenethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone; Chlorine: 2- (4-metapyridinophenethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone; and Chloroform chloride: 2 — (4 —ureidophenethyl) — 6 — (3,4—dimethoxy —-— This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm) _ — -· 1, !! --- ivtn ..... I--H (Please read the notes on the back before filling out this page) Order 475927 Printed by the Consumer Standards Cooperative of the Central Standard Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Explanation (68) Phenyl) -2,3,4,5-tetrahydrodatrapeptone 3-ketone; and pentamidine chloride: 2- (4-pentamidoaminophenethyl) -6- (3,4 _Dimethoxyphenyl)-2 ′ 3,4,5- four-gas tower coaxes a 3-ketone; and hexamethylene chloride: 2— (4-hexamethyleneaminophenethyl) -6— (3,4 A dimethoxyphenyl group) a 2,3,4,5-tetrazolium tower to cope with a 3-fluorene; and pentafluoropropanyl chloride: 2-(4 pentafluorobiamidoaminophenethyl) a 6 — (3,4-dimethoxyphenyl) _2,3,4,5-tetrahydrofluorene coaxes a 3-ketone. In a similar manner, by letting (3-aminomethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydrodatrapeptide-3 The reactants mentioned above are reacted to obtain the following products (ie, expressed as% reactants ::% products "); and acetamidine chloride: 2-(3-ammonylaminophenethyl)-6 — (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-trione, m.p. 1 0 5 °; and trifluoroacetamidine: 2— ( 3-difluoroacetamidomethyl) -6- (3'4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap well 3-ketone m.p. 13 6 ° ; This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ -I---I- · 1 -II ϋ (Please read the precautions on the back before filling this page) Order 475927 Ministry of Economic Affairs Printed by the Consumer Standards Cooperative of the Central Bureau of Standards A7 B7 V. Description of the Invention (69) and Methanesulfonate Chlorine: 2-(3-Methanesulfonylpyridyl)-6-(3,4_dimethoxyphenyl) ) A 2,3,4,5-four air tower coaxes a 3-ketone, m.p. 1 7 7 °; With propionyl chloride: 2_ (3-Hamidinaminyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrazolium tower to cope with 3-3-fluorene; m p. 1520; with dimethylpropanyl chloride: 2- (3-tert-butylcarbonylaminobenzyl) -6- (3,4-dimethoxyphenyl) -2,3, 4,5-tetrahydro-trap- 3-ketone; with butyl chloride: 2- (3-butyridinoaminobenzyl)-6- (3,4-dimethoxyphenyl)-2, 3, 4, 5 —tetrahydro-trap — 3 — ketone; and isobutyryl chloride: 2 — (3-isobutyrylamino) — 6 — (3,4-dimethoxyphenyl) — 2, 3,4,5-tetrahydropyrene-3 ketone; and methyl chloroformate: 2- (3-methoxymethoxyaminomethyl) -6- (3,4-dimethoxyphenyl) A 2,3,4,5-tetrahydrothrapy-3 ketone; and pentamidine chloride: 2- (3-pentamidineaminofluorenyl) -6- (3,4-dimethoxybenzene Base) -2,3,4,5 -tetrahydro trap -3 -one; and cyclopentane carbochloride: This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ _ ( (Please read the notes on the back before filling this page) 475927 Printed by the Consumer Standards Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A7 B7 V. Invention Description (70) 2 — (3 —Cyclopentyl Aminomethyl Narrow Base) — 6 — (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro trap-one 3-ketone; and ethyl chloroformate: 2- (3-ethoxyamidoamino) A 6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trap-3-ketone; m.p. 1 7 9 °; and chloroform:- (3-Methosamine amino narrow group)-6- (3,4-dimethoxyphenyl) -2,3,4,5-tetraazepine to coax a 3-payer; and chloroformyl chloride : 2- (3-ureidobenzyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetraaza-tower to coke 3-3-fluorene; and pentamidine chloride: 2 — (3 —pentylaminomethyl) — 6 — (3 ′ 4-dimethoxyphenyl) — 2,3,4,5 —tetrazol tower coaxing a 3 —one 1; and hexamethylene chloride: 2- (3-Hexamidineaminobenzyl)-6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydroda-well 3-ketone; and pentafluoropropanyl chloride: 2- (3-pentafluoropropanylaminomethyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrakis Hydrogen trap-3-ketone. In a similar way, by making 2- (3-aminoamino) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3 this paper size applies China National Standard (CNS) A4 specification (210X297 mm) _ 73 _ (Please read the precautions on the back before filling this page) 475927 A7 B7 V. Description of the invention (71), 4, 5-Tetrahydrotrap trap 1-3 —The ketone reacts with the following reactants to obtain the following products (ie, expressed as ~ reactants': | product #); and acetamidine chloride: 2- (3-acetamidinebenzyl) A 6- (3-cyclopentyloxy-4 4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-trap —3-one; and trifluoroacetamyl chloride: 2_ ( 3-trifluoroacetamidomethyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydrotrap-3 -Ketone, τώ.ρ · 70 °; and mesylsulfonium chloride: 2- (3-methanesulfenylbenzyl) -6— (3-cyclopentyloxy-4—methoxyphenyl) -5 —Ethyl-2,3,4,5-tetrachlorodatra-3-one; and propanyl chloride: Printed by the Consumers' Cooperative of the Central Bureau of Standards of the Ministry of Education (please read the precautions on the back before filling out this page) 2-(3 -Propanylbenzyl)-6-(3-Cyclopentyloxy-4 -Methoxy Phenyl)-5-ethyl-2,3,4,5-tetrahydro tower trap 3-ketone, mp113. ; With 2,2-dimethylpropanyl chloride: 2- (3-tert-butylaminoamino)-6- (3-cyclopentyloxy-4-methoxyphenyl) -5_ethyl 1,2,3,4,5 — Tetrahydro tower coaxing a 3-ketone; This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ 475927 A7 B7 V. Description of the invention (72) and Ding Yi Chlorine: 2- (3-butanamido-narrow) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrazolium Cake-3 ketone; and isobutylphosphonium chloride: 2- (3-isobutylamidinosyl) -6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2 , 3,4 '5-tetraazawell-a 3-ketone; and methyl chloroformate: 2- (3-methoxycarbonylaminobenzyl) -6- (3-cyclopentyloxy-4 4-methoxy Phenyl)-5 -ethyl-2,3 '4' 5 -tetrahydrophilic _ 3-ketone; and pentamidine chloride: 2-(3-pentamidine aminomethyl)-6-(3 —Cyclopentyloxy—4-methoxyphenyl) —5—ethyl—2,3,4,5-tetraaza tower trap—3-ketone; With cyclopentane carbochloride: printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) 2 — (3 —cyclopentylcarbamoyl) — 6 — (3 —Cyclopentyloxy-4 monomethoxyphenyl) —5—ethyl—2,3 ′ 4 ′ 5—tetrahydro tower to cope with 3—one; and ethyl chloroformate: 2— (3-ethoxycarbonyl Aminofluorenyl) _6- (3-cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro trap-3, one ketone, mp153 °; This paper size applies the Chinese National Standard (CNS) A4 specification (210X 297 mm) 75 475927 A7 B7 V. Description of the invention (73) and formachlor chloride: 2_ (3-formazone amino narrow base)-6- (3-Cyclopentyloxy-4-methoxyphenyl) -5-ethyl-2,3,4,5-tetrahydro-3-well; and chloroformyl chloride: 2_ (3_urea Amidino) -6- (3-cyclopentyloxy-4-methoxymethoxy) -5-ethyl-2,3,4,5-tetraazapyridine, and 3-pentanone; and pentamidine Chlorine: 2- (3-pentamylaminomethyl) -6- (3-cyclopentyloxy-1 4 —Methoxyphenyl) —5—ethyl—2,3,4,5—tetrahydropyridine—3—one; and hexamethylene chloride: 2— (3-hexamidineamino narrow group) — (3 —Cyclopentyloxy—4-monomethoxyphenyl) —5-ethyl-2,3,4,5-tetrahydro tower trap—3-ketone; and pentafluoropropanyl chloride: Employees of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the Consumer Cooperative (please read the precautions on the back before filling out this page) 2— (3-Pentafluoropropanamido narrow group) —6— (3-Cyclopentyloxy-4—methoxyphenyl) One 5-ethyl-2,3,4,5-tetrahydro 11 fluorene trap 3-ketone. Example 7 A solution of 2.4 g of 3- (3,4-dimethoxybenzoate) propionic acid dissolved in 10 Om of glacial acetic acid and 1.7 g of p-nitrobenzyl basic paper was used in China. Standard (CNS) A4 specification (210X 297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 475927 A7 ____B7 V. Description of the invention (74) Hydrazine reaction, and stirred at 100 ° C for 2 hours. The solvent was removed and the residue was treated in a manner that resulted in 2- (4-nitrobenzyl) -6 ~ (3'4-dimethoxyphenyl) -2,3,4,5-tetrakiπ Answering a 3-ketone, π · ρ · 1260 〇 In a similar way, the following compounds were obtained, which are 3- (3, 4 ~ dimethoxyformyl) propionic acid and 4-mononitrophenylhydrazine Reaction: 2- (4-nitrophenyl) -6- (3,4-dimethoxyphenyl) -2,3,4,5-tetrahydro-trapable 3-ketone. The following examples are related to pharmaceutical formulations: Example A: A solution of 100 g of the active compound of formula I and 5 g of disodium hydrogen phosphate in an injection bottle is placed in 3 times of distilled water, using 2 N Hydrochloric acid adjusted its pH to 6.5, and then filled it into an injection bottle through aseptic filtration, freeze-dried it under aseptic conditions, and sealed it aseptically. Each injection bottle contains 5 til g of active compound. Example B: A suppository is fused with 20 g of the active compound of formula I into 100 g of soybean lecithin and 1 400 g of cocoa fat. The resulting mixture is poured into a mold and left to stand. cool down. Each suppository contains 20 mg of active compound. This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) _ 77 / _ ----.------ • installed-(Please read the precautions on the back before filling this page) Order 475927 Printed by the Consumers Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A7 B7_V. Description of the Invention (75) Example C: The solution will be lg of the active compound of formula I, 9 · 38 g of N a Η 2 P 0 4 · 2 Η 2 0, 2 8.48 g of Na2HP04 • 12H20 and 0.1 g of ammonium chlorobenzyl ammonium were dissolved in 9 4 Omj? Of double distilled water. The pH of the resulting mixed solution was adjusted to 6.8 and sterilized by radiation to prepare a solution. This solution can be used as eye drops. Example D: Ointment In a sterile state, 500 mg of the active compound of formula I was mixed with 99.5 g of petrolatum. Example E: A tablet containing a mixture of 1 kg of the active compound of formula I, 4 kg of lactose, 1.2 kg of potato starch, 0.2 kg of talc and 0 1.1 kg of magnesium stearate is compressed in a conventional manner. In order to produce tablets, each tablet contains 10mg of active compound. Example F: Coated tablets In a manner similar to Example E, compressed into tablets, and then coated with a layer of sucrose, potato starch, talc, tragacanth and coloring agent in a conventional manner. 0 Example G: Capsule paper size Applicable to China National Standard (CNS) A4 specification (210X297 mm) _ ^ _ (Please read the precautions on the back before filling out this page) 475927 A7 B7__ V. Description of the invention (76) Use 2 kg of the active compound of formula I as usual The method is' filled in hard gelatin capsules so that each capsule contains 20 mg of active compound. Example IX: 1 kg of the active compound of formula I solvent 60 and secondary distilled water in an ampoule, the resulting solution was sterile diluted, filled into an ampoule, freeze-dried in a sterile state, and then sterile seal. Each ampoule contains 10 mg of active compound. ----------------- Equipment ------ Order ------ (Please read the notes on the back before filling this page) Employees of the Central Standards Bureau of the Ministry of Economic Affairs The paper size printed by the consumer cooperative is applicable to the Chinese National Standard (CNS) A4 (210X297 mm) _ 79-

Claims (1)

475927 Α8 BS C8 D8 > Attachment to the scope of the patent application of six '~ α: Physiologically acceptable finger, 2 fV R (Please read the notes on the back before filling in this page) • .......-S1 · Wherein-R 1 is Η, R 2 is Η or A, R 3 and R 4 are each independently 0 R i, R 5 is phenyl, which is mono-substituted by Re, and Q is C Bu 2 alkylene, R 6 is -NH2 '-NR8R9 or ~ n〇2, R 8 and R 9 are each independently fluorene, can be substituted by 1 to 5 gas and / or chlorine atom Fluorenyl, a co-Ci-e group, -S 0 2 A, A is Ci-e alkyl, which can be substituted by the lg atom, R 10 is eight or (5-3 cycloalkyl, And H a 5 series is fluorine, chlorine, bromine or iodine. To BB furniture standard (CNS) eighty four (210X297 mm) 0-1--1 1--1, τ al IT tku > 7 ^ fluorine and / or chlorine 475927 A8 B8 C8 D8 々, patent application scope 2 · a) 2-(4 ethoxycarbonylamino fluorenyl)-6-(3, 4 dimethyl Oxyphenyl) -2,3,4,5-tetrahydrodatrapeptone-3 monoketone; b) 2- (3-methylamine amidinoyl) -6- (3,4-dimethoxy Phenyl) -2,3,4,5-tetrahydro-trap-3-ketone; c) 2- (3-ethylamidoamidinyl) -6- (3,4-dimethoxyphenyl) One 2,3,4,5-tetrahydro tower to coax a 3-ketone; d) 2- (4-trifluoroethylamidofluorenyl) -6- (3., 4-dimethoxyphenyl) One 5-ethyl-2,3,4,5-tetrahydro tower trap one 3-ketone ·, e) 2— (4-ethoxycarbonylaminoamidino) -6— (3,4-dimethoxy Phenyl) -5 -ethyl -2,3,4,5 -tetrahydro trap -3-ketone; f) 2-(4-methoxymethoxyaminomethyl)-6-(3,4 -Dimethoxyphenyl) -5 -ethyl -2,3,4,5 -tetrahydrotrap -3 -one; g) 2-(4-butanylaminomethyl)-6- (3,4 -dimethoxyphenyl) -5 -ethyl -2,3,4,5-tetrahydrodatrapeptone -3 -one. 3. A method for preparing a compound of formula I and its plutonium as described in item 1 of the scope of the patent application, which is characterized in that the compound of formula α is free from the Chinese National Standard (CNS) Li) (Please read the notes on the back before filling in this page) -2-475927 A8 B8 C8 D8 6. Scope of patent application 11. Among them, R 1,: R 2, R 3 and R 4 are as defined in item 1 of the scope of patent application, and react with a compound of formula m R 5 — Q-X m where R 5 and Q are as As defined above, and X is chlorine, bromohydroxy or reactive esterified hydroxyl, or it is characterized by the compound D of formula IV " IV I ¥¥ I 1 才 'p p where E is hydrogen or * ^^^, and react with a compound of formula V H2N-NH-Q — RV where Q and R5 are as defined above, or It is characterized by reducing nitro, alkylating or tritiating primary or secondary amines (please read the precautions on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) 3 475927 A8 B8 C8 _08 VI. Apply for a patent scope or hydrolyze cyano group to convert the R5 group in the compound of formula I into another R 5 The group 'and / or convert the base of formula I to hydrazone by interacting with an acid. 4. A pharmaceutical composition for inhibiting phosphodiesterase IV, comprising at least one compound of the formula I as claimed in item 1 of the patent application scope and / or a physiologically acceptable tincture thereof. 5. The compound of formula I according to item 1 of the scope of patent application and its physiologically acceptable peptone are used for the treatment of inflammatory processes, allergies, asthma and autoimmune diseases. '6. If the compound of formula I and its physiologically acceptable peptone in item 1 of the scope of patent application are used as phosphodiesterase IV inhibitors. (Please read the precautions on the reverse side before filling out this page) One pack., AT .f i sound r I 1 talents The size of this paper is in accordance with China National Standards (CNS) A4 (210X297 mm)